Design, Synthesis and Biological Evaluation of Highly Selective CDK9 Inhibitors for Cancer Treatment

Design, Synthesis and Biological Evaluation of Highly Selective CDK9 Inhibitors for Cancer Treatment PDF Author: Hao Shao
Publisher:
ISBN:
Category : Cyclin-dependent kinases
Languages : en
Pages : 0

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Design, Synthesis and Biological Evaluation of Highly Selective CDK9 Inhibitors for Cancer Treatment

Design, Synthesis and Biological Evaluation of Highly Selective CDK9 Inhibitors for Cancer Treatment PDF Author: Hao Shao
Publisher:
ISBN:
Category : Cyclin-dependent kinases
Languages : en
Pages : 0

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Design, Synthesis, and Optimisation of Highly Selective Macrocyclic CDK9 Inhibitors

Design, Synthesis, and Optimisation of Highly Selective Macrocyclic CDK9 Inhibitors PDF Author: Rui Gao
Publisher:
ISBN:
Category :
Languages : en
Pages :

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Privileged Structures in Drug Discovery

Privileged Structures in Drug Discovery PDF Author: Larry Yet
Publisher: John Wiley & Sons
ISBN: 1118686357
Category : Medical
Languages : en
Pages : 562

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Book Description
A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.

Coumarin and Its Derivatives

Coumarin and Its Derivatives PDF Author: Maria João Matos
Publisher: Mdpi AG
ISBN: 9783036527758
Category : Science
Languages : en
Pages : 416

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Book Description
Coumarins are widely distributed in nature and can be found in a large number of naturally occurring and synthetic bioactive molecules. The unique and versatile oxygen-containing heterocyclic structure makes them a privileged scaffold in Medicinal Chemistry. Many coumarin derivatives have been extracted from natural sources, designed, synthetized, and evaluated on different pharmacological targets. In addition, coumarin-based ion receptors, fluorescent probes, and biological stains are growing quickly and have extensive applications to monitor timely enzyme activity, complex biological events, as well as accurate pharmacological and pharmacokinetic properties in living cells. The extraction, synthesis, and biological evaluation of coumarins have become extremely attractive and rapidly developing topics. A large number of research and review papers have compiled information on this important family of compounds in 2020. Research articles, reviews, communications, and concept papers focused on the multidisciplinary profile of coumarins, highlighting natural sources, most recent synthetic pathways, along with the main biological applications and theoretical studies, were the main focus of this book. The huge and growing range of applications of coumarins described in this book is a demonstration of the potential of this family of compounds in Organic Chemistry, Medicinal Chemistry, and different sciences related to the study of natural products. This book includes 23 articles: 17 original papers and six review papers.

Fragment-Based Drug Discovery

Fragment-Based Drug Discovery PDF Author: Steven Howard
Publisher: Royal Society of Chemistry
ISBN: 1782625658
Category : Medical
Languages : en
Pages : 314

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Book Description
Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.

Kinomics

Kinomics PDF Author: Heinz-Bernhard Kraatz
Publisher: John Wiley & Sons
ISBN: 3527337652
Category : Science
Languages : en
Pages : 364

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Book Description
Das umfassende Referenzwerk zur Kinase-Forschung: Ausführlich werden die Themen Kinase-Engineering, Peptidsubstrat-Engineering, das Design von Co-Substraten und Kinasehemmer erläutert sowie deren Anwendung in der Bio- und Pharmaforschung beschrieben.

Discovery and Development of Anti-Breast Cancer Agents from Natural Products

Discovery and Development of Anti-Breast Cancer Agents from Natural Products PDF Author: Goutam Brahmachari
Publisher: Elsevier
ISBN: 0128212780
Category : Science
Languages : en
Pages : 386

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Book Description
Discovery and Development of Anti-Breast Cancer Agents from Natural Products presents cutting-edge research advances in the field of bioactive natural products and natural drug formulations. This volume in the Natural Products Drug Discovery series focuses on molecules of natural origin and their synthetic analogs that show promising potential to act as anti-breast cancer and chemotherapeutic agents. Combining foundational background information on cancer mechanisms with details of medicinal structures from natural products, this volume compiles the latest developments from across interdisciplinary fields. Discovery and Development of Anti-Breast Cancer Agents from Natural Products will serve as a valuable resource for researchers working to discover promising leads for the development of novel pharmaceuticals for breast cancer, highlighting a number of key structures from natural products and exploring possible future developments in the area. Highlights active agents from natural sources for development as novel anti-cancer agents Features contributions from active researchers and leading experts working in the field Includes foundational background information on both breast cancer mechanisms and natural product structures to support researchers from different disciplines

Burger's Medicinal Chemistry, Drug Discovery, and Development, Set

Burger's Medicinal Chemistry, Drug Discovery, and Development, Set PDF Author: Donald J. Abraham
Publisher: Wiley
ISBN:
Category : Science
Languages : en
Pages : 6356

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Book Description
Now in its seventh edition, Burger's Medicinal Chemistry, Drug Discovery and Development provides an established, recognized, authoritative and comprehensive source on medicinal chemistry and drug discovery and development. This flagship reference for medicinal chemists and pharmaceutical professions has been thoroughly updated and expanded across 8 volumes to incorporate the entire process of drug development (preclinical testing, clinical trials, etc.) alongside the traditional strengths in medicinal chemistry and drug discovery.

Next Generation Kinase Inhibitors

Next Generation Kinase Inhibitors PDF Author: Paul Shapiro
Publisher: Springer Nature
ISBN: 3030482839
Category : Medical
Languages : en
Pages : 224

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Book Description
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.

HIV-1 Integrase

HIV-1 Integrase PDF Author: Nouri Neamati
Publisher: John Wiley & Sons
ISBN: 1118015363
Category : Science
Languages : en
Pages : 710

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Book Description
This book comprehensively covers the mechanisms of action and inhibitor design for HIV-1 integrase. It serves as a resource for scientists facing challenging drug design issues and researchers in antiviral drug discovery. Despite numerous review articles and isolated book chapters dealing with HIV-1 integrase, there has not been a single source for those working to devise anti-AIDS drugs against this promising target. But this book fills that gap and offers a valuable introduction to the field for the interdisciplinary scientists who will need to work together to design drugs that target HIV-1 integrase.