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.


For students, researchers and industrialists in the field of medicinal chemistry

Table of Contents

Preface (B.E. Maryanoff, A.B. Reitz). Novel peptide mimetic building blocks and strategies for efficient lead finding (D. Obrecht et al.). Recent advances in the medicinal chemistry of taxoid anticancer agents (I. Ojima et al.). Synthesis and structure-activity relationships of peroxidic antimalarials based on artemisinin (M.A. Avery et al.). Design of compound libraries for detecting and pursuing novel small molecule leads (A.M. Ferguson, R.D. Cramer). A theoretical model of the human thrombin receptor (PAR-1), the first known protease-activated G-protein-coupled receptor (M.P. Beavers et al.). Farnesyl transferase inhibitors: design of a new class of cancer chemotherapeutic agents (T.M. Williams, C.J. Dinsmore).


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© 1999
Elsevier Science
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