| bioorganic & medicinal chemistry letters: Targeted Protein Degradation Angela M. Cacace, Christopher M. Hickey, Miklós Békés, 2021-08-26 This volume contains a collection of innovative techniques for studying targeted protein degradation. Chapters guide readers through heterobifunctional proteolysis-targeting chimeras (PROTACs) approaches, E3 ligase, E3 ligase-induced ubiquitylation, proteomic approaches, novel degrader molecules, molecular glue, and stabilize binding interaction between a target and E3 ubiquitin ligase. Written in the format of the highly successful Methods in Molecular Biology series, each chapter includes an introduction to the topic, lists necessary materials and reagents, includes tips on troubleshooting and known pitfalls, and step-by-step, readily reproducible protocols. Authoritative and cutting-edge, Targeted Protein Degradation: Methods and Protocols aims to ensure successful results in this emerging field of drug discovery. |
| bioorganic & medicinal chemistry letters: Exercise, Nutrition and the Older Woman Maria A. Fiatarone Singh, 2000-04-21 Exercise, Nutrition and the Older Woman: Wellness for Women Over Fifty is a comprehensive guide to the major wellness issues for women over fifty. The author is a physician who explores diet, exercise and lifestyle choices from a medical perspective. The book assists in the design and implementation of programs to optimize good health and quality o |
| bioorganic & medicinal chemistry letters: Quantitative Structure-Activity Relationships in Drug Design, Predictive Toxicology, and Risk Assessment Roy, Kunal, 2015-02-28 Quantitative structure-activity relationships (QSARs) represent predictive models derived from the application of statistical tools correlating biological activity or other properties of chemicals with descriptors representative of molecular structure and/or property. Quantitative Structure-Activity Relationships in Drug Design, Predictive Toxicology, and Risk Assessment discusses recent advancements in the field of QSARs with special reference to their application in drug development, predictive toxicology, and chemical risk analysis. Focusing on emerging research in the field, this book is an ideal reference source for industry professionals, students, and academicians in the fields of medicinal chemistry and toxicology. |
| bioorganic & medicinal chemistry letters: Comparative Qsar James Devillers, 1998-03-03 As the 21st century approaches, there is little doubt that the tools and resources are available to unlock all the secrets of Quantitative Structure-Activity Relationships (QSAR) in order to design more efficient drugs and safer chemicals. The comparison QSAR models provide are a key to reach a deep understanding of the foundation and a better optimisation of the use of these statistical tools. Seeking out the similarities and differences among QSAR Models allows the user to estimate their simulation performances, find chemo-taxonomical links, and uncover In vivo/In Vitro relationships. The purpose of this book is to highlight the multifaceted aspect of the term comparative QSAR by bringing together QSAR experts of various origins and allowing them to offer their views on this diverse subject. |
| bioorganic & medicinal chemistry letters: Bioisosteres in Medicinal Chemistry Nathan Brown, 2012-06-18 Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section. |
| bioorganic & medicinal chemistry letters: Anticancer Agents Iwao Ojima, 2001 Anticancer Agents: Frontiers in Cancer Chemotherapy describes cutting-edge approaches in the development of anticancer agents for chemotherapy. |
| bioorganic & medicinal chemistry letters: Scaffold Hopping in Medicinal Chemistry Nathan Brown, 2013-11-06 This first systematic treatment of the concept and practice of scaffold hopping shows the tricks of the trade and provides invaluable guidance for the reader's own projects. The first section serves as an introduction to the topic by describing the concept of scaffolds, their discovery, diversity and representation, and their importance for finding new chemical entities. The following part describes the most common tools and methods for scaffold hopping, whether topological, shape-based or structure-based. Methods such as CATS, Feature Trees, Feature Point Pharmacophores (FEPOPS), and SkelGen are discussed among many others. The final part contains three fully documented real-world examples of successful drug development projects by scaffold hopping that illustrate the benefits of the approach for medicinal chemistry. While most of the case studies are taken from medicinal chemistry, chemical and structural biologists will also benefit greatly from the insights presented here. |
| bioorganic & medicinal chemistry letters: Fragment-based Drug Discovery Daniel A. Erlanson, Wolfgang Jahnke, 2016-02-23 From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets. |
| bioorganic & medicinal chemistry letters: N-Heterocycles Keshav Lalit Ameta, Ravi Kant, Andrea Penoni, Angelo Maspero, Luca Scapinello, 2022-04-23 This book presents an overview of the recent advancements for the synthesis of small- and medium-sized azaheterocycles, including pyrroles, indoles, pyrimidines, pyridines, pyrrolidines, imidazoles, pyrazoles, pyrazolines, lactams, and 1,2,3-triazoles, which are significant scaffolds for compounds with pharmaceutical uses. The book also discusses various properties and performance attributes of azaheterocycles including their bioactivity and synthetic strategies. Given the contents, the book will be a valuable reference for students, researchers, and professionals interested in organic synthesis and medicinal chemistry. |
| bioorganic & medicinal chemistry letters: Lead Generation Jörg Holenz, 2016-03-16 In this comprehensive two-volume resource on the topic senior lead generation medicinal chemists present a coherent view of the current methods and strategies in industrial and academic lead generation. This is the first book to combine both standard and innovative approaches in comparable breadth and depth, including several recent successful lead generation case studies published here for the first time. Beginning with a general discussion of the underlying principles and strategies, individual lead generation approaches are described in detail, highlighting their strengths and weaknesses, along with all relevant bordering disciplines like e.g. target identification and validation, predictive methods, molecular recognition or lead quality matrices. Novel lead generation approaches for challenging targets like DNA-encoded library screening or chemical biology approaches are treated here side by side with established methods as high throughput and affinity screening, knowledge- or fragment-based lead generation, and collaborative approaches. Within the entire book, a very strong focus is given to highlight the application of the presented methods, so that the reader will be able to learn from real life examples. The final part of the book presents several lead generation case studies taken from different therapeutic fields, including diabetes, cardiovascular and respiratory diseases, neuroscience, infection and tropical diseases. The result is a prime knowledge resource for medicinal chemists and for every scientist involved in lead generation. |
| bioorganic & medicinal chemistry letters: Chemistry and Applications of Benzimidazole and its Derivatives Maria Marinescu, 2019-10-02 Finding new strategies for synthesizing benzimidazole derivatives and functionalizing the benzimidazole core has proved to be important due to the compound's various applications in medicine, chemistry, and other areas. The multitude of benzimidazole derivatives marketed as drugs has led to intensive research in the field for the discovery of new biologically active structures. The general applications of benzimidazole derivatives in materials chemistry, electronics, technology, dyes, pigments, and agriculture open up new research horizons. This book guides the rational design of benzimidazole derivatives synthesis with certain applications. Chapters cover such topics as therapeutic use of benzimidazole in conditions like diabetes, viruses, and parasitic diseases; X-ray crystal structure of selected benzimidazole derivatives; benzimidazole compounds for cancer therapy; and others. |
| bioorganic & medicinal chemistry letters: In Silico Modeling of Drugs Against Coronaviruses Kunal Roy, 2021 This essential volume explores a variety of tools and protocols of structure-based (homology modeling, molecular docking, molecular dynamics, protein-protein interaction network) and ligand-based (pharmacophore mapping, quantitative structure-activity relationships or QSARs) drug design for ranking and prioritization of candidate molecules in search of effective treatment strategy against coronaviruses. Beginning with an introductory section that discusses coronavirus interactions with humanity and COVID-19 in particular, the book then continues with sections on tools and methodologies, literature reports and case studies, as well as online tools and databases that can be used for computational anti-coronavirus drug research. Written for the Methods in Pharmacology and Toxicology series, chapters include the kind of practical detail and implementation advice that ensures high quality results in the lab. Comprehensive and timely, In Silico Modeling of Drugs Against Coronaviruses: Computational Tools and Protocols is an ideal reference for researchers working on the development of novel anti-coronavirus drugs for SARS-CoV-2 and for coronaviruses that will likely appear in the future. |
| bioorganic & medicinal chemistry letters: Structural Biology in Drug Discovery Jean-Paul Renaud, 2020-01-09 With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins |
| bioorganic & medicinal chemistry letters: Artificial Intelligence in Drug Design Alexander Heifetz, 2022-11-05 This volume looks at applications of artificial intelligence (AI), machine learning (ML), and deep learning (DL) in drug design. The chapters in this book describe how AI/ML/DL approaches can be applied to accelerate and revolutionize traditional drug design approaches such as: structure- and ligand-based, augmented and multi-objective de novo drug design, SAR and big data analysis, prediction of binding/activity, ADMET, pharmacokinetics and drug-target residence time, precision medicine and selection of favorable chemical synthetic routes. How broadly are these approaches applied and where do they maximally impact productivity today and potentially in the near future. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modeling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique, Artificial Intelligence in Drug Design is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists and drug designers. |
| bioorganic & medicinal chemistry letters: Comprehensive Natural Products III , 2020-07-22 Comprehensive Natural Products III, Third Edition, Seven Volume Set updates and complements the previous two editions, including recent advances in cofactor chemistry, structural diversity of natural products and secondary metabolites, enzymes and enzyme mechanisms and new bioinformatics tools. Natural products research is a dynamic discipline at the intersection of chemistry and biology concerned with isolation, identification, structure elucidation, and chemical characteristics of naturally occurring compounds such as pheromones, carbohydrates, nucleic acids and enzymes. This book reviews the accumulated efforts of chemical and biological research to understand living organisms and their distinctive effects on health and medicine and to stimulate new ideas among the established natural products community. Provides readers with an in-depth review of current natural products research and a critical insight into the future direction of the field Bridges the gap in knowledge by covering developments in the field since the second edition published in 2010 Split into 7 sections on key topics to allow students, researchers and professionals to find relevant information quickly and easily Ensures that the knowledge within is easily understood by and applicable to a large audience |
| bioorganic & medicinal chemistry letters: Green Chemistry Hosam El-Din M. Saleh, Martin Koller, 2018-02-28 To an increasing extent, green chemistry is a new chemical and engineering approach of chemistry and engineering, dedicated to make manufacturing processes and our world as a whole more sustainable world with a growing tendency. Green chemistry approaches are based on ecofriendly technologies, aiming to reduce or eliminate the use of solvents, or render them efficient and safer. Moreover, this scientific field is devoted to reduction or elimination of prevailing environmental and health threats, which typically accompany chemical products and traditional processes. The present book Green Chemistry contains 9 selected chapters, starting with a general introductory chapter on green chemistry, and covers many recent applications and developments based on the principles of green chemistry. This book is considered the appropriate way to communicate the advances in green materials and their applications to the scientific community. Chemists, scientists and researchers from related areas, and undergraduates involved in environmental issues and interested in approaches to improve the quality of life could find an inspiring and effective guide by reading this book. |
| bioorganic & medicinal chemistry letters: Organic Synthesis Belakatte Parameshwarappa Nandeshwarappa, 2020-05-27 The book ‘Organic Synthesis - A Nascent Relook’ is a compendium of the recent progress in all aspects of organic chemistry including bioorganic chemistry, organo-metallic chemistry, asymmetric synthesis, heterocyclic chemistry, natural product chemistry, catalytic, green chemistry and medicinal chemistry, polymer chemistry, as well as analytical methods in organic chemistry. The book presents the latest developments in these fields. The chapters are written by chosen experts who are internationally known for their eminent research contributions. Organic synthesis is the complete chemical synthesis of a target molecule. In this book, special emphasis is given to the synthesis of various bioactive heterocycles. Careful selection of various topics in this book will serve the rightful purpose for the chemistry community and the industrial houses at all levels. |
| bioorganic & medicinal chemistry letters: Advances in Medicinal Chemistry B.E. Maryanoff, A.B. Reitz, 1999-04-01 Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment of malaria based on the natural product artemisinin. Chapter 4 applies computational chemistry to the evaluation of compound libraries for biological testing. Chapter 5 describes the construction of a 3-dimensional molecular model of the human thrombin receptor, the first protease-activated G-protein coupled receptor (PAR-1), as a means to explore the intermolecular contacts involved in agonist peptide recognition. Finally, Chapter 6 describes the research conducted at Merck on inhibitors of farnesyl transferase as a potential treatment for human cancers. |
| bioorganic & medicinal chemistry letters: Cannabinoids As Therapeutic Agents Raphael Mechoulam, 2019-06-13 Published in 1986: The plant Cannabis sativa L. and its numerous preparations have been used as therapeutic agents for millenia. In the present book, the editor has tried to summarize the use in the past, to present an overview of modern research and applications to predict future developments. |
| bioorganic & medicinal chemistry letters: Nitric Oxide Donors Peng George Wang, Tingwei Bill Cai, Naoyuki Taniguchi, 2005-08-16 Nitric oxide is a highly potent regulatory molecule with great pharmaceutical potential. This handbook fills a real gap in combining the chemistry of nitric oxide releasing substances with their practical applications in biology and drug design. It covers all classes of nitric oxide donors, from organic nitrates to nitroso compounds, guanidines and metal-NO complexes. In addition to a detailed treatment of the chemistry of NO donors, numerous examples of successful diagnostic and pharmacological applications are discussed, as well as further therapeutic targets for these substances. |
| bioorganic & medicinal chemistry letters: Camptothecins New Anticancer Agents Milan Potmesil, Herbert M. Pinedo, 1994-12-19 This exciting new book presents the first comprehensive overview of clinical trials of camptothecins, a new class of anticancer agents. Camptothecins are synthetic and semisynthetic derivatives of a plant alkaloid that inhibit a cellular enzyme and trigger a cascade of events leading to programmed cell death. Special attention is given to the adverse effects of camptothecin treatment, as well as to prevention and control. The book boasts contributions by some of the most respected authorities in camptothecin research, who have Conducted much of the pre-clinical work which helped to renew interest in camptothecins Discovered and identified the natural product camptothecin and synthesized most of the anlogues Discovered the mechanism of camptothecin cytotoxicity |
| bioorganic & medicinal chemistry letters: Modern Organic Synthesis George S. Zweifel, Michael H. Nantz, Peter Somfai, 2017-03-13 This book bridges the gap between sophomore and advanced / graduate level organic chemistry courses, providing students with a necessary background to begin research in either an industry or academic environment. • Covers key concepts that include retrosynthesis, conformational analysis, and functional group transformations as well as presents the latest developments in organometallic chemistry and C–C bond formation • Uses a concise and easy-to-read style, with many illustrated examples • Updates material, examples, and references from the first edition • Adds coverage of organocatalysts and organometallic reagents |
| bioorganic & medicinal chemistry letters: Quinazolinone and Quinazoline Derivatives Ali Gamal Al-kaf, 2020 |
| bioorganic & medicinal chemistry letters: Axially Chiral Compounds Bin Tan, 2021-11-22 Axially Chiral Compounds Explore this comprehensive and current volume summarizing the characteristics, synthesis, and applications of axial chirality Appearing widely in natural products, biologically active molecules, asymmetric chemistry, and material science, axially chiral motifs constitute the core backbones of the majority of chiral ligands and organocatalysts in asymmetric catalysis. In a new work of particular relevance to synthetic chemists, Axially Chiral Compounds: Asymmetric Synthesis and Applications delivers a clearly structured and authoritative volume covering the classification, characteristics, synthesis, and applications of axial chirality. A must read for every synthetic chemist practicing today, the book follows the development history, research status, and applications of axial chirality. An introductory chapter familiarizes the reader with foundational material before the distinguished authors describe the different classes and the synthesis of axial chiral compounds used in asymmetric synthesis. The book concludes with a focus on the applications of chiral ligands, chiral catalysts, and materials. Readers will also benefit from the inclusion of: A thorough introduction to asymmetric synthesis, including biaryls atropisomers, heterobiaryls atropisomers, and non-biaryls atropisomers Explorations of chiral allene, spiro skeletons, and natural products Practical discussions of asymmetric transformation, chiral ligands, and chiral catalysts An examination of miscellaneous applications of axially chiral compounds Perfect for organic chemists, chemists working with or on organometallics, catalytic chemists, and materials scientists, Axially Chiral Compounds: Asymmetric Synthesis and Applications will also earn a place in the libraries of natural products chemists who seek a one-stop reference for compounds exhibiting axial chirality. |
| bioorganic & medicinal chemistry letters: Anticancer Agents Qiao-Hong Chen, 2021-03-02 This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers. |
| bioorganic & medicinal chemistry letters: Vector-Borne Diseases David Claborn, Sujit Bhattacharya, Syamal Roy, 2020-06-03 Vector-Borne Diseases - Recent Developments in Epidemiology and Control utilizes the unique capabilities of open-access publishing to share exciting developments in the biology, diagnosis, and treatment of diseases spread by arthropods. From malaria to dengue to leishmaniasis, the diseases addressed in this book continue to present threats to the life and well-being of millions around the world. The international cast of writers published here provide specific insight into a full spectrum of diseases spread by insects and their close relatives. |
| bioorganic & medicinal chemistry letters: Peroxisomes in Biology and Medicine H. Dariush Fahimi, Helmut Sies, 2012-12-06 |
| bioorganic & medicinal chemistry letters: Dengue and Zika: Control and Antiviral Treatment Strategies Rolf Hilgenfeld, Subhash G. Vasudevan, 2018-05-29 This contributed volume contains 25 chapters from leading international scientists working on dengue and Zika viruses, who came together in Praia do Tofo in Mozambique to discuss the latest developments in the fields of epidemiology, pathogenesis, structural virology, immunology, antiviral drug discovery and development, vaccine efficacy, and mosquito control programs. The meeting venue offered an opportunity to discuss current research on these flaviviruses in an idyllic setting, and also to develop first-hand appreciation of the issues in infectious diseases facing developing countries and of the research gaps in Africa. For readers, who should include basic and clinical researchers in the field and public health professionals, the chapters are organized to provide a comprehensive overview of the various topics in current dengue and Zika virus research. A unique feature of the proceedings of this meeting is the inclusion of the discussions that took place following presentations. These have been transcribed and appended to the end of the relevant chapters, and they form the “salt in the soup” of this book. |
| bioorganic & medicinal chemistry letters: Kinesins and Cancer Frank Kozielski, FSB, 2015-03-02 This interdisciplinary volume collates research work on kinesins and cancer. Authors attempt to validate members of the kinesin superfamily as potential targets for drug development in cancer chemotherapy. The work begins by highlighting the importance of kinesins, summarising current knowledge and how they are shown to be crucial for mitosis. Chapters go on to explore how this family of proteins are emerging as a novel target for chemotherapeutic intervention and drug development. Readers will learn how kinesins travel along microtubules to fulfill their many roles in intracellular transport or cell division. Several compounds that inhibit two mitotic kinesins (called Eg5 and CENP-E) have entered Phase I and II clinical trials and are explored in these chapters. Additional mitotic kinesins are currently being validated as drug targets, raising the possibility that the repertoire of kinesin-based drug targets may expand in the future. The book is suitable as a reference standard for the field of kinesins and cancer. It will interest those in academia and pharmaceutical companies, and anyone with an interest in the medical relevance of these proteins, which cutting edge methodologies are now enabling us to understand in astonishing detail. |
| bioorganic & medicinal chemistry letters: The SAGE Handbook of Geographical Knowledge John A Agnew, David N Livingstone, 2011-02-17 A refreshingly innovative approach to charting geographical knowledge. A wide range of authors trace the social construction and contestation of geographical ideas through the sites of their production and their relational geographies of engagement. This creative and comprehensive book offers an extremely valuable tool to professionals and students alike. - Victoria Lawson, University of Washington A Handbook that recasts geograph′s history in original, thought-provoking ways. Eschewing the usual chronological march through leading figures and big ideas, it looks at geography against the backdrop of the places and institutional contexts where it has been produced, and the social-cum-intellectual currents underlying some of its most important concepts. - Alexander B. Murphy, University of Oregon The SAGE Handbook of Geographical Knowledge is a critical inquiry into how geography as a field of knowledge has been produced, re-produced, and re-imagined. It comprises three sections on geographical orientations, geography′s venues, and critical geographical concepts and controversies. The first provides an overview of the genealogy of geography. The second highlights the types of spatial settings and locations in which geographical knowledge has been produced. The third focuses on venues of primary importance in the historical geography of geographical thought. Orientations includes chapters on: Geography - the Genealogy of a Term; Geography′s Narratives and Intellectual History Geography′s Venues includes chapters on: Field; Laboratory; Observatory; Archive; Centre of Calculation; Mission Station; Battlefield; Museum; Public Sphere; Subaltern Space; Financial Space; Art Studio; Botanical/Zoological Gardens; Learned Societies Critical concepts and controversies - includes chapters on: Environmental Determinism; Region; Place; Nature and Culture; Development; Conservation; Geopolitics; Landscape; Time; Cycle of Erosion; Time; Gender; Race/Ethnicity; Social Class; Spatial Analysis; Glaciation; Ice Ages; Map; Climate Change; Urban/Rural. Comprehensive without claiming to be encyclopedic, textured and nuanced, this Handbook will be a key resource for all researchers with an interest in the pasts, presents and futures of geography. |
| bioorganic & medicinal chemistry letters: Catalytic Antibodies Ehud Keinan, 2006-03-06 Exploiting the inherent combinatorial mechanism in the biosynthesis of antibodies, an almost limitless variety of biocatalysts may be generated. Catalytic antibodies are capable of performing almost any type of reaction with high selectivity and stereospecificity. Here, the pioneers in the use of catalytic antibodies review the entire scope of this interdisciplinary field, covering such topics as: * theoretical aspects of structure, mechanism and kinetics * practical considerations, from immunization techniques to screening methods * in vitro evolution and other modern approaches * applications from organic synthesis to medical uses. Backed by the leading authorities in antibody catalysis, this is the first book to provide such comprehensive coverage and constitutes a prime reference for biochemists, organic chemists, biotechnologists and biomedical researchers. |
| bioorganic & medicinal chemistry letters: Cytochrome P-450 Paul Ortiz De Monetllano, 1986-03 Major advances have been made in recent years in clarifying the molecular properties of the cytochrome P-450 system. These advances stem, in practical terms, from the generally recognized importance of cytochrome P-450 in the metabolism of drugs and in the bioactivation of xenobiotics to toxic products. The fascinating multiplicity and differential regulation of cytochrome P-450 isozymes, and their ability to catalyze extraordinarily difficult chemical transformations, have independently drawn many chemists and biochemists into the P-450 circle. Progress in the field, from a technical point of view, has been propelled by the de velopment of reliable procedures for the purification of membrane-bound enzymes, by the growing repertoire of molecular biological techniques, and by the development of chemical models that mimic the catalytic action of P-450. As a result, our understanding of the P-450 system is moving from the descriptive, pharmacological level into the tangible realm of atomic detail. The rapid progress and multidisciplinary character of the cytochrome P-450 field, which cuts across the lines that traditionally divide disciplines as diverse as inorganic chemistry and genetics, have created a need for an up-to-date evaluation of the advances that have been made. It is hoped that this book, with its molecular focus on the cytochrome P-450 system, will alleviate this need. The authors of the individual chapters have strived to emphasize recent results without sacrificing the background required to make their chapters comprehensible to informed nonspecialists. |
| bioorganic & medicinal chemistry letters: Diversity-Oriented Synthesis Andrea Trabocchi, 2013-06-17 Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications. |
| bioorganic & medicinal chemistry letters: Megatastic: Space Academy Top That! Publishing PLC, 2002-12-01 |
| bioorganic & medicinal chemistry letters: Transactions of the Royal Historical Society: Volume 24 Ian W. Archer, 2014-11-27 Transactions of the Royal Historical Society is an annual collection of major articles representing some of the best historical research by some of the world's most distinguished historians. Volume 24 of the sixth series includes the following articles: 'Educating the Nation I: Schools', 'The 'Feudal Revolution' and the Origins of Italian City Communes', 'Preachers and Hearers in Revolutionary London: Contextualising Parliamentary Fast Sermons', ''The Honest Tradesman's Honour': Occupational and Social Identity in Seventeenth-Century England', 'Andres Bello and the Challenges of Spanish American Liberalism', 'Skill, Craft, and Histories of Industrialisation in Europe and Asia', 'Christendom's Bulwark: Croatian Identity and the Response to the Ottoman Advance, Fifteenth to Sixteenth Centuries', 'Croats and Croatia in the Wake of the Great War', 'Dissimilation, Assimilation, and the Unmixing of Peoples: German and Croatian Scholars Working towards a New Ethno-Polical Order, 1919-45'. |
| bioorganic & medicinal chemistry letters: Radical SAM Enzymes , 2018-08-09 Radical SAM Enzymes, Volume 606, the latest release in the Methods in Enzymology series, highlights new advances in the field, with this new volume presenting interesting chapters on the Characterization of the glycyl radical enzyme choline trimethylamine-lyase and its radical S-adenosylmethionine activating enzyme, Diphathimide biosynthesis, Radical SAM glycyl radical activating enzymes, Radical SAM enzyme BioB in the biosynthesis of biotin, Biogenesis of the PQQ cofactor, Role of MoaAC in the biogenesis of the molybdenum cofactor, Biosynthesis of the nitrogenase cofactor, Bioinformatics of the radical SAM superfamily, The involvement of SAM radical enzymes in the biosynthesis of methanogenic coenzymes, methanopterin and coenzyme F420, and more. |
| bioorganic & medicinal chemistry letters: Chemical Proteomics Gerard Drewes, Marcus Bantscheff, 2011-11-08 The multidisciplinary science of chemical proteomics studies how small molecules of synthetic or natural origin bind to proteins and modulate their function. In Chemical Proteomics: Methods and Protocols, expert researchers in the field provide key techniques to investigate chemical proteomics focusing on analytical strategies, how probes are generated, techniques for the discovery of small molecule targets and the probing of target function, and small molecule ligand and drug discovery. Written in the highly successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and key tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Chemical Proteomics : Methods and Protocols seeks to provide methodologies that will contribute to a wider application of chemical proteomics methods in biochemical and cell biological laboratories. |
| bioorganic & medicinal chemistry letters: Knovel Critical Tables Knovel Corporation, 2003 |
| bioorganic & medicinal chemistry letters: Heterocycles B. P. Nandeshwarappa, 2020-06 |
| bioorganic & medicinal chemistry letters: Instant Lessons in Music Michael Redman, 2002 Photocopiable pre-prepared lessons in music covering practical work and theory and includes games, research, revision and testing activities suitable for junior high school classes. |
| bioorganic medicinal chemistry letters: Bioisosteres in Medicinal Chemistry Nathan Brown, 2012-06-18 Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section. |
| bioorganic medicinal chemistry letters: Targeted Protein Degradation Angela M. Cacace, Christopher M. Hickey, Miklós Békés, 2021-08-26 This volume contains a collection of innovative techniques for studying targeted protein degradation. Chapters guide readers through heterobifunctional proteolysis-targeting chimeras (PROTACs) approaches, E3 ligase, E3 ligase-induced ubiquitylation, proteomic approaches, novel degrader molecules, molecular glue, and stabilize binding interaction between a target and E3 ubiquitin ligase. Written in the format of the highly successful Methods in Molecular Biology series, each chapter includes an introduction to the topic, lists necessary materials and reagents, includes tips on troubleshooting and known pitfalls, and step-by-step, readily reproducible protocols. Authoritative and cutting-edge, Targeted Protein Degradation: Methods and Protocols aims to ensure successful results in this emerging field of drug discovery. |
| bioorganic medicinal chemistry letters: Quantitative Structure-Activity Relationships in Drug Design, Predictive Toxicology, and Risk Assessment Roy, Kunal, 2015-02-28 Quantitative structure-activity relationships (QSARs) represent predictive models derived from the application of statistical tools correlating biological activity or other properties of chemicals with descriptors representative of molecular structure and/or property. Quantitative Structure-Activity Relationships in Drug Design, Predictive Toxicology, and Risk Assessment discusses recent advancements in the field of QSARs with special reference to their application in drug development, predictive toxicology, and chemical risk analysis. Focusing on emerging research in the field, this book is an ideal reference source for industry professionals, students, and academicians in the fields of medicinal chemistry and toxicology. |
| bioorganic medicinal chemistry letters: Exercise, Nutrition and the Older Woman Maria A. Fiatarone Singh, 2000-04-21 Exercise, Nutrition and the Older Woman: Wellness for Women Over Fifty is a comprehensive guide to the major wellness issues for women over fifty. The author is a physician who explores diet, exercise and lifestyle choices from a medical perspective. The book assists in the design and implementation of programs to optimize good health and quality o |
| bioorganic medicinal chemistry letters: Comparative Qsar James Devillers, 1998-03-03 As the 21st century approaches, there is little doubt that the tools and resources are available to unlock all the secrets of Quantitative Structure-Activity Relationships (QSAR) in order to design more efficient drugs and safer chemicals. The comparison QSAR models provide are a key to reach a deep understanding of the foundation and a better optimisation of the use of these statistical tools. Seeking out the similarities and differences among QSAR Models allows the user to estimate their simulation performances, find chemo-taxonomical links, and uncover In vivo/In Vitro relationships. The purpose of this book is to highlight the multifaceted aspect of the term comparative QSAR by bringing together QSAR experts of various origins and allowing them to offer their views on this diverse subject. |
| bioorganic medicinal chemistry letters: Scaffold Hopping in Medicinal Chemistry Nathan Brown, 2013-11-06 This first systematic treatment of the concept and practice of scaffold hopping shows the tricks of the trade and provides invaluable guidance for the reader's own projects. The first section serves as an introduction to the topic by describing the concept of scaffolds, their discovery, diversity and representation, and their importance for finding new chemical entities. The following part describes the most common tools and methods for scaffold hopping, whether topological, shape-based or structure-based. Methods such as CATS, Feature Trees, Feature Point Pharmacophores (FEPOPS), and SkelGen are discussed among many others. The final part contains three fully documented real-world examples of successful drug development projects by scaffold hopping that illustrate the benefits of the approach for medicinal chemistry. While most of the case studies are taken from medicinal chemistry, chemical and structural biologists will also benefit greatly from the insights presented here. |
| bioorganic medicinal chemistry letters: Anticancer Agents Iwao Ojima, 2001 Anticancer Agents: Frontiers in Cancer Chemotherapy describes cutting-edge approaches in the development of anticancer agents for chemotherapy. |
| bioorganic medicinal chemistry letters: Fragment-based Drug Discovery Daniel A. Erlanson, Wolfgang Jahnke, 2016-02-23 From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets. |
| bioorganic medicinal chemistry letters: Plant Bioactives and Drug Discovery Valdir Cechinel-Filho, 2012-05-22 An in-depth exploration of the applications of plant bioactive metabolites in drug research and development Highlighting the complexity and applications of plant bioactive metabolites in organic and medicinal chemistry, Plant Bioactives and Drug Discovery: Principles, Practice, and Perspectives provides an in-depth overview of the ways in which plants can inform drug research and development. An edited volume featuring multidisciplinary international contributions from acclaimed scientists researching bioactive natural products, the book provides an incisive overview of one of the most important topics in pharmaceutical studies today. With coverage of strategic methods of natural compound isolation, structural manipulation, natural products in clinical trials, quality control, and more, and featuring case studies on medicinal plants, the book serves as a definitive guide to the field of plant biodiversity as it relates to medicine. In addition, chapters on using natural products as drugs that target specific disease areas, including neurological disorders, inflammation, infectious diseases, and cancer, illustrate the myriad possibilities for therapeutic applications. Wide ranging and comprehensive, Plant Bioactives and Drug Discovery also includes important information on marketing, regulations, intellectual property rights, and academic-industry collaboration as they relate to plant-based drug research, making it an essential resource for advanced students and academic and industry professionals working in biochemical, pharmaceutical, and related fields. |
| bioorganic medicinal chemistry letters: Chemometrics and Cheminformatics in Aquatic Toxicology Kunal Roy, 2022-01-06 CHEMOMETRICS AND CHEMINFORMATICS IN AQUATIC TOXICOLOGY Explore chemometric and cheminformatic techniques and tools in aquatic toxicology Chemometrics and Cheminformatics in Aquatic Toxicology delivers an exploration of the existing and emerging problems of contamination of the aquatic environment through various metal and organic pollutants, including industrial chemicals, pharmaceuticals, cosmetics, biocides, nanomaterials, pesticides, surfactants, dyes, and more. The book discusses different chemometric and cheminformatic tools for non-experts and their application to the analysis and modeling of toxicity data of chemicals to various aquatic organisms. You’ll learn about a variety of aquatic toxicity databases and chemometric software tools and webservers as well as practical examples of model development, including illustrations. You’ll also find case studies and literature reports to round out your understanding of the subject. Finally, you’ll learn about tools and protocols including machine learning, data mining, and QSAR and ligand-based chemical design methods. Readers will also benefit from the inclusion of: A thorough introduction to chemometric and cheminformatic tools and techniques, including machine learning and data mining An exploration of aquatic toxicity databases, chemometric software tools, and webservers Practical examples and case studies to highlight and illustrate the concepts contained within the book A concise treatment of chemometric and cheminformatic tools and their application to the analysis and modeling of toxicity data Perfect for researchers and students in chemistry and the environmental and pharmaceutical sciences, Chemometrics and Cheminformatics in Aquatic Toxicology will also earn a place in the libraries of professionals in the chemical industry and regulators whose work involves chemometrics. |
| bioorganic medicinal chemistry letters: Chemistry and Applications of Benzimidazole and its Derivatives Maria Marinescu, 2019-10-02 Finding new strategies for synthesizing benzimidazole derivatives and functionalizing the benzimidazole core has proved to be important due to the compound's various applications in medicine, chemistry, and other areas. The multitude of benzimidazole derivatives marketed as drugs has led to intensive research in the field for the discovery of new biologically active structures. The general applications of benzimidazole derivatives in materials chemistry, electronics, technology, dyes, pigments, and agriculture open up new research horizons. This book guides the rational design of benzimidazole derivatives synthesis with certain applications. Chapters cover such topics as therapeutic use of benzimidazole in conditions like diabetes, viruses, and parasitic diseases; X-ray crystal structure of selected benzimidazole derivatives; benzimidazole compounds for cancer therapy; and others. |
| bioorganic medicinal chemistry letters: Lead Generation Jörg Holenz, 2016-03-16 In this comprehensive two-volume resource on the topic senior lead generation medicinal chemists present a coherent view of the current methods and strategies in industrial and academic lead generation. This is the first book to combine both standard and innovative approaches in comparable breadth and depth, including several recent successful lead generation case studies published here for the first time. Beginning with a general discussion of the underlying principles and strategies, individual lead generation approaches are described in detail, highlighting their strengths and weaknesses, along with all relevant bordering disciplines like e.g. target identification and validation, predictive methods, molecular recognition or lead quality matrices. Novel lead generation approaches for challenging targets like DNA-encoded library screening or chemical biology approaches are treated here side by side with established methods as high throughput and affinity screening, knowledge- or fragment-based lead generation, and collaborative approaches. Within the entire book, a very strong focus is given to highlight the application of the presented methods, so that the reader will be able to learn from real life examples. The final part of the book presents several lead generation case studies taken from different therapeutic fields, including diabetes, cardiovascular and respiratory diseases, neuroscience, infection and tropical diseases. The result is a prime knowledge resource for medicinal chemists and for every scientist involved in lead generation. |
| bioorganic medicinal chemistry letters: Artificial Intelligence in Drug Design Alexander Heifetz, 2022-11-05 This volume looks at applications of artificial intelligence (AI), machine learning (ML), and deep learning (DL) in drug design. The chapters in this book describe how AI/ML/DL approaches can be applied to accelerate and revolutionize traditional drug design approaches such as: structure- and ligand-based, augmented and multi-objective de novo drug design, SAR and big data analysis, prediction of binding/activity, ADMET, pharmacokinetics and drug-target residence time, precision medicine and selection of favorable chemical synthetic routes. How broadly are these approaches applied and where do they maximally impact productivity today and potentially in the near future. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary software and tools, step-by-step, readily reproducible modeling protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and unique, Artificial Intelligence in Drug Design is a valuable resource for structural and molecular biologists, computational and medicinal chemists, pharmacologists and drug designers. |
| bioorganic medicinal chemistry letters: In Silico Modeling of Drugs Against Coronaviruses Kunal Roy, 2021 This essential volume explores a variety of tools and protocols of structure-based (homology modeling, molecular docking, molecular dynamics, protein-protein interaction network) and ligand-based (pharmacophore mapping, quantitative structure-activity relationships or QSARs) drug design for ranking and prioritization of candidate molecules in search of effective treatment strategy against coronaviruses. Beginning with an introductory section that discusses coronavirus interactions with humanity and COVID-19 in particular, the book then continues with sections on tools and methodologies, literature reports and case studies, as well as online tools and databases that can be used for computational anti-coronavirus drug research. Written for the Methods in Pharmacology and Toxicology series, chapters include the kind of practical detail and implementation advice that ensures high quality results in the lab. Comprehensive and timely, In Silico Modeling of Drugs Against Coronaviruses: Computational Tools and Protocols is an ideal reference for researchers working on the development of novel anti-coronavirus drugs for SARS-CoV-2 and for coronaviruses that will likely appear in the future. |
| bioorganic medicinal chemistry letters: N-Heterocycles Keshav Lalit Ameta, Ravi Kant, Andrea Penoni, Angelo Maspero, Luca Scapinello, 2022-04-23 This book presents an overview of the recent advancements for the synthesis of small- and medium-sized azaheterocycles, including pyrroles, indoles, pyrimidines, pyridines, pyrrolidines, imidazoles, pyrazoles, pyrazolines, lactams, and 1,2,3-triazoles, which are significant scaffolds for compounds with pharmaceutical uses. The book also discusses various properties and performance attributes of azaheterocycles including their bioactivity and synthetic strategies. Given the contents, the book will be a valuable reference for students, researchers, and professionals interested in organic synthesis and medicinal chemistry. |
| bioorganic medicinal chemistry letters: Green Chemistry Hosam El-Din M. Saleh, Martin Koller, 2018-02-28 To an increasing extent, green chemistry is a new chemical and engineering approach of chemistry and engineering, dedicated to make manufacturing processes and our world as a whole more sustainable world with a growing tendency. Green chemistry approaches are based on ecofriendly technologies, aiming to reduce or eliminate the use of solvents, or render them efficient and safer. Moreover, this scientific field is devoted to reduction or elimination of prevailing environmental and health threats, which typically accompany chemical products and traditional processes. The present book Green Chemistry contains 9 selected chapters, starting with a general introductory chapter on green chemistry, and covers many recent applications and developments based on the principles of green chemistry. This book is considered the appropriate way to communicate the advances in green materials and their applications to the scientific community. Chemists, scientists and researchers from related areas, and undergraduates involved in environmental issues and interested in approaches to improve the quality of life could find an inspiring and effective guide by reading this book. |
| bioorganic medicinal chemistry letters: Comprehensive Natural Products III , 2020-07-22 Comprehensive Natural Products III, Third Edition, Seven Volume Set updates and complements the previous two editions, including recent advances in cofactor chemistry, structural diversity of natural products and secondary metabolites, enzymes and enzyme mechanisms and new bioinformatics tools. Natural products research is a dynamic discipline at the intersection of chemistry and biology concerned with isolation, identification, structure elucidation, and chemical characteristics of naturally occurring compounds such as pheromones, carbohydrates, nucleic acids and enzymes. This book reviews the accumulated efforts of chemical and biological research to understand living organisms and their distinctive effects on health and medicine and to stimulate new ideas among the established natural products community. Provides readers with an in-depth review of current natural products research and a critical insight into the future direction of the field Bridges the gap in knowledge by covering developments in the field since the second edition published in 2010 Split into 7 sections on key topics to allow students, researchers and professionals to find relevant information quickly and easily Ensures that the knowledge within is easily understood by and applicable to a large audience |
| bioorganic medicinal chemistry letters: Structural Biology in Drug Discovery Jean-Paul Renaud, 2020-01-09 With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins |
| bioorganic medicinal chemistry letters: Modern Organic Synthesis George S. Zweifel, Michael H. Nantz, Peter Somfai, 2017-03-13 This book bridges the gap between sophomore and advanced / graduate level organic chemistry courses, providing students with a necessary background to begin research in either an industry or academic environment. • Covers key concepts that include retrosynthesis, conformational analysis, and functional group transformations as well as presents the latest developments in organometallic chemistry and C–C bond formation • Uses a concise and easy-to-read style, with many illustrated examples • Updates material, examples, and references from the first edition • Adds coverage of organocatalysts and organometallic reagents |
| bioorganic medicinal chemistry letters: Axially Chiral Compounds Bin Tan, 2021-11-22 Axially Chiral Compounds Explore this comprehensive and current volume summarizing the characteristics, synthesis, and applications of axial chirality Appearing widely in natural products, biologically active molecules, asymmetric chemistry, and material science, axially chiral motifs constitute the core backbones of the majority of chiral ligands and organocatalysts in asymmetric catalysis. In a new work of particular relevance to synthetic chemists, Axially Chiral Compounds: Asymmetric Synthesis and Applications delivers a clearly structured and authoritative volume covering the classification, characteristics, synthesis, and applications of axial chirality. A must read for every synthetic chemist practicing today, the book follows the development history, research status, and applications of axial chirality. An introductory chapter familiarizes the reader with foundational material before the distinguished authors describe the different classes and the synthesis of axial chiral compounds used in asymmetric synthesis. The book concludes with a focus on the applications of chiral ligands, chiral catalysts, and materials. Readers will also benefit from the inclusion of: A thorough introduction to asymmetric synthesis, including biaryls atropisomers, heterobiaryls atropisomers, and non-biaryls atropisomers Explorations of chiral allene, spiro skeletons, and natural products Practical discussions of asymmetric transformation, chiral ligands, and chiral catalysts An examination of miscellaneous applications of axially chiral compounds Perfect for organic chemists, chemists working with or on organometallics, catalytic chemists, and materials scientists, Axially Chiral Compounds: Asymmetric Synthesis and Applications will also earn a place in the libraries of natural products chemists who seek a one-stop reference for compounds exhibiting axial chirality. |
| bioorganic medicinal chemistry letters: Quinazolinone and Quinazoline Derivatives Ali Gamal Al-kaf, 2020 |
| bioorganic medicinal chemistry letters: Vector-Borne Diseases David Claborn, Sujit Bhattacharya, Syamal Roy, 2020-06-03 Vector-Borne Diseases - Recent Developments in Epidemiology and Control utilizes the unique capabilities of open-access publishing to share exciting developments in the biology, diagnosis, and treatment of diseases spread by arthropods. From malaria to dengue to leishmaniasis, the diseases addressed in this book continue to present threats to the life and well-being of millions around the world. The international cast of writers published here provide specific insight into a full spectrum of diseases spread by insects and their close relatives. |
| bioorganic medicinal chemistry letters: Vascular-Targeted Therapies in Oncology Dietmar W. Siemann, 2006 Vascular-Targeted Therapies in Oncology provides an interesting insight to the current status and future potential of vascular-disrupting approaches in cancer management. Emphasis is placed on target development, preclinical assessment, and the use of such targeted approaches in combination with conventional treatment regimens and the current clinical status of these therapies. |
| bioorganic medicinal chemistry letters: Anticancer Agents Qiao-Hong Chen, 2021-03-02 This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers. |
| bioorganic medicinal chemistry letters: Nitric Oxide Donors Peng George Wang, Tingwei Bill Cai, Naoyuki Taniguchi, 2005-08-16 Nitric oxide is a highly potent regulatory molecule with great pharmaceutical potential. This handbook fills a real gap in combining the chemistry of nitric oxide releasing substances with their practical applications in biology and drug design. It covers all classes of nitric oxide donors, from organic nitrates to nitroso compounds, guanidines and metal-NO complexes. In addition to a detailed treatment of the chemistry of NO donors, numerous examples of successful diagnostic and pharmacological applications are discussed, as well as further therapeutic targets for these substances. |
| bioorganic medicinal chemistry letters: The SAGE Handbook of Geographical Knowledge John A Agnew, David N Livingstone, 2011-02-17 A refreshingly innovative approach to charting geographical knowledge. A wide range of authors trace the social construction and contestation of geographical ideas through the sites of their production and their relational geographies of engagement. This creative and comprehensive book offers an extremely valuable tool to professionals and students alike. - Victoria Lawson, University of Washington A Handbook that recasts geograph′s history in original, thought-provoking ways. Eschewing the usual chronological march through leading figures and big ideas, it looks at geography against the backdrop of the places and institutional contexts where it has been produced, and the social-cum-intellectual currents underlying some of its most important concepts. - Alexander B. Murphy, University of Oregon The SAGE Handbook of Geographical Knowledge is a critical inquiry into how geography as a field of knowledge has been produced, re-produced, and re-imagined. It comprises three sections on geographical orientations, geography′s venues, and critical geographical concepts and controversies. The first provides an overview of the genealogy of geography. The second highlights the types of spatial settings and locations in which geographical knowledge has been produced. The third focuses on venues of primary importance in the historical geography of geographical thought. Orientations includes chapters on: Geography - the Genealogy of a Term; Geography′s Narratives and Intellectual History Geography′s Venues includes chapters on: Field; Laboratory; Observatory; Archive; Centre of Calculation; Mission Station; Battlefield; Museum; Public Sphere; Subaltern Space; Financial Space; Art Studio; Botanical/Zoological Gardens; Learned Societies Critical concepts and controversies - includes chapters on: Environmental Determinism; Region; Place; Nature and Culture; Development; Conservation; Geopolitics; Landscape; Time; Cycle of Erosion; Time; Gender; Race/Ethnicity; Social Class; Spatial Analysis; Glaciation; Ice Ages; Map; Climate Change; Urban/Rural. Comprehensive without claiming to be encyclopedic, textured and nuanced, this Handbook will be a key resource for all researchers with an interest in the pasts, presents and futures of geography. |
| bioorganic medicinal chemistry letters: Catalytic Antibodies Ehud Keinan, 2006-03-06 Exploiting the inherent combinatorial mechanism in the biosynthesis of antibodies, an almost limitless variety of biocatalysts may be generated. Catalytic antibodies are capable of performing almost any type of reaction with high selectivity and stereospecificity. Here, the pioneers in the use of catalytic antibodies review the entire scope of this interdisciplinary field, covering such topics as: * theoretical aspects of structure, mechanism and kinetics * practical considerations, from immunization techniques to screening methods * in vitro evolution and other modern approaches * applications from organic synthesis to medical uses. Backed by the leading authorities in antibody catalysis, this is the first book to provide such comprehensive coverage and constitutes a prime reference for biochemists, organic chemists, biotechnologists and biomedical researchers. |
| bioorganic medicinal chemistry letters: Next Generation Kinase Inhibitors Paul Shapiro, 2020-07-14 Protein kinases are fascinating enzymes that maintain the proper function of nearly every task performed by the cells of the human body. By extracting a phosphate from the energy molecule ATP and linking it to another protein, protein kinases alter the structure and ultimate function of other proteins. In this way, protein kinases help monitor the extracellular environment and integrate signaling cues that, for the most part, are beneficial for human health and survival. However, protein kinases are often dysregulated and responsible for the initiation and progression of many types of cancers, inflammatory disorders, and other diseases. Thus, decades of research have revealed much about how protein kinases are regulated and approaches to inhibit these enzymes to treat disease. However, nearly 30 years since the identification of the first clinically beneficial small molecule protein kinase inhibitor, there are only a few examples where these drugs provide sustained and durable patient responses. The goal of this book is to provide biomedical scientists, graduate, and professional degree students insight into different approaches using small molecules to block specific protein kinase functions that promote disease. |
| bioorganic medicinal chemistry letters: Prodrugs and Targeted Delivery Jarkko Rautio, 2011-01-11 This topical reference and handbook addresses the chemistry, pharmacology, toxicology and the patentability of prodrugs, perfectly mirroring the integrated approach prevalent in today's drug design. It summarizes current experiences and strategies for the rational design of prodrugs, beginning at the early stages of the development process, as well as discussing organ- and site-selective prodrugs. Every company employing medicinal chemists will be interested in this practice-oriented overview of a key strategy in modern drug discovery and development. |
| bioorganic medicinal chemistry letters: Chemical Proteomics Gerard Drewes, Marcus Bantscheff, 2011-11-08 The multidisciplinary science of chemical proteomics studies how small molecules of synthetic or natural origin bind to proteins and modulate their function. In Chemical Proteomics: Methods and Protocols, expert researchers in the field provide key techniques to investigate chemical proteomics focusing on analytical strategies, how probes are generated, techniques for the discovery of small molecule targets and the probing of target function, and small molecule ligand and drug discovery. Written in the highly successful Methods in Molecular BiologyTM series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and key tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Chemical Proteomics : Methods and Protocols seeks to provide methodologies that will contribute to a wider application of chemical proteomics methods in biochemical and cell biological laboratories. |
| bioorganic medicinal chemistry letters: Radical SAM Enzymes , 2018-08-09 Radical SAM Enzymes, Volume 606, the latest release in the Methods in Enzymology series, highlights new advances in the field, with this new volume presenting interesting chapters on the Characterization of the glycyl radical enzyme choline trimethylamine-lyase and its radical S-adenosylmethionine activating enzyme, Diphathimide biosynthesis, Radical SAM glycyl radical activating enzymes, Radical SAM enzyme BioB in the biosynthesis of biotin, Biogenesis of the PQQ cofactor, Role of MoaAC in the biogenesis of the molybdenum cofactor, Biosynthesis of the nitrogenase cofactor, Bioinformatics of the radical SAM superfamily, The involvement of SAM radical enzymes in the biosynthesis of methanogenic coenzymes, methanopterin and coenzyme F420, and more. |
| bioorganic medicinal chemistry letters: Transactions of the Royal Historical Society: Volume 24 Ian W. Archer, 2014-11-27 Transactions of the Royal Historical Society is an annual collection of major articles representing some of the best historical research by some of the world's most distinguished historians. Volume 24 of the sixth series includes the following articles: 'Educating the Nation I: Schools', 'The 'Feudal Revolution' and the Origins of Italian City Communes', 'Preachers and Hearers in Revolutionary London: Contextualising Parliamentary Fast Sermons', ''The Honest Tradesman's Honour': Occupational and Social Identity in Seventeenth-Century England', 'Andres Bello and the Challenges of Spanish American Liberalism', 'Skill, Craft, and Histories of Industrialisation in Europe and Asia', 'Christendom's Bulwark: Croatian Identity and the Response to the Ottoman Advance, Fifteenth to Sixteenth Centuries', 'Croats and Croatia in the Wake of the Great War', 'Dissimilation, Assimilation, and the Unmixing of Peoples: German and Croatian Scholars Working towards a New Ethno-Polical Order, 1919-45'. |
| bioorganic medicinal chemistry letters: Knovel Critical Tables Knovel Corporation, 2003 |
| bioorganic medicinal chemistry letters: Megatastic: Space Academy Top That! Publishing PLC, 2002-12-01 |
| bioorganic medicinal chemistry letters: Walking on the Wild Side Pat Dewil, 2008 |
| bioorganic medicinal chemistry letters: Radicals in Organic Synthesis Bernd Giese, 1986 |
| bioorganic medicinal chemistry letters: Peptide Synthesis Waleed M. Hussein, Mariusz Skwarczynski, Istvan Toth, 2019-12-27 This book provides a variety of procedures for synthetically producing peptides and their derivatives, ensuring the kind of precision that is of paramount importance for successful synthesis. Numerous techniques relevant to drugs and vaccines are explored, such as conjugation and condensation methodologies. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, Peptide Synthesis: Methods and Protocols serves as an essential guide to the many crucial processes that will allow researchers to efficiently prepare, purify, characterize, and use peptides for chemical, biochemical, and biological studies. |
| bioorganic medicinal chemistry letters: Heterocycles B. P. Nandeshwarappa, 2020-06 |
| bioorganic medicinal chemistry letters: Quinoxalines, Volume 61, Spplement 2 Desmond J. Brown, Edward C. Taylor, Jonathan A. Ellman, 2004-01-22 This volume in the Chemistry of Heterocyclic Compounds series presents a comprehensive review of the quinoxaline literature from 1975 to the present (2002), updating Volumes 5 and 35. It provides an alphabetical table of known simple quinoxalines, including new compounds discussed in this volume and their physical data, as well as the pyrazines from the original volumes. Biological activities, spectral or other physical studies, and other such materials appear at appropriate points in the text. The in-depth coverage includes synthesis, reactions, spectroscopic, and physical properties for each class of compounds. Chemistry of Heterocyclic Compounds, Volume 61: Supplement II provides the most up-to-date summation of knowledge of the synthetic chemistry of quinoxalines. |
| bioorganic medicinal chemistry letters: Antibody-Drug Conjugates L. Nathan Tumey, 2020 This volume looks at key methodologies that are commonly used across antibody drug conjugates (ADCs) programs. The chapters in this book cover topics such as conjugations to endogenous cysteine residues; click chemistry conjugations; antibody conjugations via glycosyl remodeling; analysis of ADCs by native mass spectrometry; characterization of ADCs by capillary electrophoresis; LC/MS methods for studying lysosomal ADC catabolism; and determination of ADC concentration by ligand-binding assays. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and practical, Antibody-Drug Conjugates: Methods and Protocols is a valuable resource that aims to lower the activation barrier when undertaking a new discipline, and provides a toolbox for the next generation of ADC scientists. |
Bioorganic & Medicinal Chemistry Letters
Jul 7, 2024 · Galanthamine derivatives are known for their AChE inhibitory activity. Among them, galanthamine has been approved for treatment of Alzheimer’s disease. N …
Bioorganic & Medicinal Chemistry Letters
Here, we report the binding mode of another, more polar, LC kinetic stabilizer chemotype, 3,5-substituted hydantoins.
Bioorganic & Medicinal Chemistry Letters
In this brief review, we aim at providing a general coverage of all the chemical functionalisation routes and strategies employed for the fabrication of these bioactive molecule/graphene conju …
Bioorganic & Medicinal Chemistry Letters
Here biological activity of 3-oxo-c-costic acid (1), previously isolated from Chiliadenus montanus, as well as new sesquiterpenes (2–5) and the known derivative, 3-oxoeudesma-1,4,11(13)-trien …
Bioorganic & Medicinal Chemistry Letters - CIMAP
Indanones and related compounds are important bioactive mol-ecules. These compounds have been studied for various biological activities including cancer and Alzheimer’s type of diseases.
Bioorganic & Medicinal Chemistry Letters
Here we describe the concept and demonstration of a photoactivatable pro-tein labeling technology. This technology, dubbed SPRAY (singlet oxygen activated pro-tein labeling, …
Bioorganic & Medicinal Chemistry Letters - Columbia University
To overcome this limitation, we designed ketone-based functionalities capable of forming reversible covalent adducts, while displaying high meta-bolic stability, and imparting improved …
Bioorganic & Medicinal Chemistry Letters
In the present work, we report the synthesis of 1,4-disubstituted 1,2,3-triazoles and 1,2,4-triazolo[1, 5-a]pyrimidine deriva-tives via copper (I)-catalyzed azide-alkyne cycloaddition …
Bioorganic & Medicinal Chemistry Letters
We describe the exploration of N1-aryl-substituted benzimidazoles as ligands for the hepatitis C virus (HCV) internal ribosome entry site (IRES) RNA. The design of the compounds was …
Bioorganic & Medicinal Chemistry Letters
Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl Study on one-pot four-component synthesis of 9-aryl-hexahydro-acridine-1,8-diones using SiO2–I as …
Bioorganic & Medicinal Chemistry Letters
This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain …
Bioorganic & Medicinal Chemistry Letters
Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl
Bioorganic & Medicinal Chemistry Letters
In this study, we compared two perylene monoimide derivatives, PM1 and PM2, with the well-studied perylene diimide derivative, PIPER, and the well-studied porphyrin derivative, …
Bioorganic & Medicinal Chemistry Letters - PETA
Herein we report the discovery of a novel oxindole-based series of vasopressin 1b (V1b) receptor antagonists. Introducing a substituted piperazine moiety and optimizing the southern and the …
Bioorganic & Medicinal Chemistry Letters
Several small molecule EZH2 inhibitors with different chemotypes have been reported in the literature, many of which use a bicyclic heteroaryl core. Herein, we report the design and …
Bioorganic & Medicinal Chemistry Letters
Bioorganic & Medicinal Chemistry Letters journal homepage: www.elsevier.com/locate/bmcl
Bioorganic & Medicinal Chemistry Letters
Proteomics has emerged as an important tool in unraveling the intricate, dynamic nature of many cellular processes.1 The preva-lence of protein–protein interactions (PPIs) in signal …
Bioorganic & Medicinal Chemistry Letters
We report the synthesis and use of methyl N-(tert-butoxycarbonyl)pyridine-2-carbimidothioate as new reagent for the preparation of N-phenylpyridinecarboxamidines (“arylimidamides”), a class …
Bioorganic & Medicinal Chemistry Letters - CORE
Protein misfolding is an emerging field that crosses multiple therapeutic areas and causes many serious diseases. As the biological pathways of protein misfolding become more clearly …
Bioorganic & Medicinal Chemistry Letters
Here, we report for the first time a series of curcuminoid derivatives that enhance telomerase activity in an in vitro telomerase assay. The structures of these compounds are shown in …
Bioorganic & Medicinal Chemistry Letters
Jul 7, 2024 · Galanthamine derivatives are known for their AChE inhibitory activity. Among them, galanthamine has been approved for treatment of …
Bioorganic & Medicinal Chemistry Letters
Here, we report the binding mode of another, more polar, LC kinetic stabilizer chemotype, 3,5-substituted hydantoins.
Bioorganic & Medicinal Chemistry Letters
In this brief review, we aim at providing a general coverage of all the chemical functionalisation routes and strategies employed for the fabrication of …
Bioorganic & Medicinal Chemistry Letters
Here biological activity of 3-oxo-c-costic acid (1), previously isolated from Chiliadenus montanus, as well as new sesquiterpenes (2–5) and the known …
Bioorganic & Medicinal Chemistry Letters - CIMAP
Indanones and related compounds are important bioactive mol-ecules. These compounds have been studied for …
