Advances in Medicinal Chemistry ( Volume 4 )

Publication series :Volume 4

Author: Maryanoff   B. E.;Reitz   A. B.  

Publisher: Elsevier Science‎

Publication year: 1999

E-ISBN: 9780080526379

P-ISBN(Paperback): 9780762300648

P-ISBN(Hardback):  9780762300648

Subject: R914 pharmaceutical chemistry

Language: ENG

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Description

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.

Chapter

Front Cover

pp.:  1 – 4

Copyright Page

pp.:  5 – 6

CONTENTS

pp.:  6 – 8

LIST OF CONTRIBUTORS

pp.:  8 – 10

PREFACE

pp.:  10 – 12

CHAPTER 2. RECENT ADVANCES IN THE MEDICINAL CHEMISTRY OF TAXOID ANTICANCER AGENTS

pp.:  80 – 136

CHAPTER 3. SYNTHESIS AND STRUCTURE–ACTIVITY RELATIONSHIPS OF PEROXIDIC ANTIMALARIALS BASED ON ARTEMISININ

pp.:  136 – 230

CHAPTER 4. DESIGN OF COMPOUND LIBRARIES FOR DETECTING AND PURSUING NOVEL SMALL MOLECULE LEADS

pp.:  230 – 256

CHAPTER 5. A THEORETICAL MODEL OF THE HUMAN THROMBIN RECEPTOR (PAR-1), THE FIRST KNOWN PROTEASE-ACTIVATED G-PROTEIN-COUPLED RECEPTOR

pp.:  256 – 284

CHAPTER 6. FARNESYL TRANSFERASE INHIBITORS: DESIGN OF A NEW CLASS OF CANCER CHEMOTHERAPEUTIC AGENTS

pp.:  284 – 326

INDEX

pp.:  326 – 339

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