Combinatorial Library Design and Evaluation, Ghose, Arup
Название: Anticancer Agents: Design, Synthesis and Evaluation ISBN: 3036501401 ISBN-13(EAN): 9783036501406 Издательство: Неизвестно Рейтинг: Цена: 147040.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание:
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.
Автор: Perovitch, Milosh Название: Radiological Evaluation Of The Spinal Cord ISBN: 0367260867 ISBN-13(EAN): 9780367260866 Издательство: Taylor&Francis Рейтинг: Цена: 153120.00 T Наличие на складе: Поставка под заказ. Описание: First Published in 1989, this book explores the relationship between plants and insects and the ways in which they interact with each other. Carefully compiled and filled with a vast repertoire of notes, diagrams, and references this book serves as a useful reference for students of oncology, and other practitioners in their respective fields.
Автор: S.R. Walker; C. Lumley; N. McAuslane Название: The Relevance of Ethnic Factors in the Clinical Evaluation of Medicines ISBN: 9401046212 ISBN-13(EAN): 9789401046213 Издательство: Springer Рейтинг: Цена: 46570.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание: The mutual acceptance of foreign clinical data would reduce the time and resources required to develop a new medicine for the international market by eliminating the requirement for the routine repetition of clinical studies in local populations.
Автор: Ghose, Arup Viswanadhan, Vellerkad Название: Combinatorial library design and evaluation ISBN: 0367397226 ISBN-13(EAN): 9780367397227 Издательство: Taylor&Francis Рейтинг: Цена: 65320.00 T Наличие на складе: Поставка под заказ. Описание: This text traces developments in rational drug discovery and combinatorial library design with contributions from 50 leading scientists in academia and industry who offer coverage of basic principles, design strategies, methodologies, software tools and algorithms, and applications. It outlines the fundamentals of pharmacophore modelling and 3D Quantitative Structure-Activity Relationships (QSAR), classical QSAR, and target protein structure-based design methods.
Автор: W.H. Moos; M.R. Pavia; B.K. Kay; Andrew D. Ellingt Название: Annual Reports in Combinatorial Chemistry and Molecular Diversity ISBN: 9072199235 ISBN-13(EAN): 9789072199232 Издательство: Springer Рейтинг: Цена: 213360.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание: Drug discovery - better, faster, cheaper? Indeed, more compounds have been made and screened in the 1990s than in the last hundred years of pharmaceutical research. This first volume covers: combinatorial chemistry, combinatorial biology and evolution, and informatics and related topics.
Название: High-Throughput Lead Optimization in Drug Discovery ISBN: 0367387719 ISBN-13(EAN): 9780367387716 Издательство: Taylor&Francis Рейтинг: Цена: 65320.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание:
A Single Source on Parallel Synthesis for Lead Optimization
The end of the previous millennium saw an explosion in the application of parallel synthesis techniques for making compounds for high-throughput screening. Over time, it became clear that more thought in the design phase of library development is necessary to generate high quality hits. More recently, the use of parallel synthesis techniques has shifted to applications beyond screening collections. Exploring the nuances of this technology, High-Throughput Lead Optimization in Drug Discovery describes the application of parallel synthesis to lead optimization and the design and synthesis of targeted libraries.
Examine Case Studies that Cover a Range of Different Biological Targets
Featuring real-world examples and contributions from well-known scientists, the book explores the shift to conducting parallel lead optimization in-house while outsourcing most of the screening libraries synthesis. It includes more than 15 case studies that encompass a range of biological targets for application in different therapeutic areas. The text contains examples of solid and solution-phase techniques for the synthesis of directed libraries. The chapter authors explain the design principles they used to direct the choice of templates and diversity elements.
Speed Up Drug Discovery and the Hit-to-Lead Process
Focusing on the application of combinatorial chemistry to medicinal chemistry, this volume compiles a series of optimization projects that give you a snapshot of successes and challenges in the use of parallel synthesis for lead optimization. It explores how this technology, when applied to library design, can speed up drug discovery.
Автор: Babaev Название: Incorporation of Heterocycles into Combinatorial Chemistry ISBN: 3319500139 ISBN-13(EAN): 9783319500133 Издательство: Springer Рейтинг: Цена: 51230.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание: The author has summarized a decade of teaching combinatorial chemistry into this timely brief. The solid phase synthesis of unnatural heterocyclic alpha-amino acids is illustrated by practical examples starting from the ABCs of peptide synthesis explored in chapter one. Chapter two is concerned with the solid phase synthesis which is shown on various techniques – BillBoard, tea-bag, and Lantern devices, and demonstrated on heterocyclic examples and protocols. In the third chapter the tools for accelerating chemical synthesis – solid phase and liquid phase – are reviewed. Here the techniques of parallel refluxing (including microwave and flow technique) and parallel separation (filtration, centrifugation, evaporation, and chromatography) are described. In the chapters 4 and 5 the author goes on to describe how the liquid phase synthesis of heterocycles (reductive amination and Ugi reaction of heterocycles) is illustrated with the use of semi-automated protocols. Finally, the design of combinatorial libraries of heterocycles is reviewed including the original author’s findings.
Название: Optimization of solid-phase combinatorial synthesis ISBN: 036739653X ISBN-13(EAN): 9780367396534 Издательство: Taylor&Francis Рейтинг: Цена: 65320.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание: "Addresses the key topic in combinatorial synthesis--how to optimize the quality of a combinatorial library--by determining the usefulness of synthesized compunds, the reliability of biological assay results, and analyzing acadmic and industrial applications, real-world examples, and case studies of successful and unsuccessful technologies."
Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has allowed scientists to generate a range of new molecular structures from natural products and observe how they interact with biological targets. Combinatorial Synthesis of Natural Product-Based Libraries summarizes the most important perspectives on the application of combinatorial chemistry and natural products to novel drug discovery.
The book details the latest approaches for implementing combinatorial research and testing methodologies to the synthesis of natural product-based libraries. Interconnecting the important aspects of this emerging field through the work of several leading scientists, it covers the computational analysis of natural molecules and details strategies for designing compound libraries, using bioinformatics in particular. The authors describe numerous synthetic methods for producing natural products and their analogs, including engineered biosynthesis and polymer-supported reagents. They also discuss additional considerations for generating libraries, such as screening, scaffolding, and yield optimization. Other chapters examine specific classes of libraries derived from natural products including carbohydrates, polyketides, peptides, alkaloids, terpenoids, steroids, flavonoids, and fungal compounds. Drawing attention to the interplay of drug discovery, natural products, and organic synthesis, Combinatorial Synthesis of Natural Product-Based Libraries contains the most recent and significant methods used to search and assess new compounds for their ability to mitigate biological processes that may lead to improved treatments for various diseases.
Автор: Kshirsagar, Tushar Название: High-Throughput Lead Optimization in Drug Discovery ISBN: 0849372682 ISBN-13(EAN): 9780849372681 Издательство: Taylor&Francis Рейтинг: Цена: 193950.00 T Наличие на складе: Поставка под заказ.
Автор: A.N. Worden; D.V. Parke; J. Marks Название: The Future of Predictive Safety Evaluation ISBN: 9401079366 ISBN-13(EAN): 9789401079365 Издательство: Springer Рейтинг: Цена: 81050.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание: Reproduction and fetal development in humans and experimental animals may be adversely affected by a wide range of drugs and environmental agents.
Автор: Dietrich Schuppan; Anthony D. Dayan; Frances A. Ch Название: The Contribution of Acute Toxicity Testing to the Evaluation of Pharmaceuticals ISBN: 3642703925 ISBN-13(EAN): 9783642703928 Издательство: Springer Рейтинг: Цена: 130610.00 T Наличие на складе: Есть у поставщика Поставка под заказ. Описание: International Symposium. IFPMA Symposium, Geneva 30-31 October 1984
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