Combinatorial Chemistry and Molecular

Combinatorial Chemistry and Molecular Diversity in Drug Discovery is one of the first comprehensive books to cover this explosive area. It is must reading for medicinal chemists, pharmacologists, molecular biologists, biochemists, enzymologists, and drug discovery research managers in industry, academia, and government.

Eric M. Gordon and James F. Kerwin are the authors of Combinatorial Chemistry and Molecular Diversity in Drug Discovery, published by Wiley.

Foreword: Combinatorial Chemistry at a Crossroads

ix

(8)

Walter H. Moos, MitoKor, San Diego, California

Preface

xvii

(4)

Contributors

xxi

PART I. Combinatorial Chemistry and Molecular Diversity: An Introduction

1

(178)

1. Historical Overview of the Developing Field of Molecular Diversity

3

(14)

John C. Chabala, Pharmacopeia Inc., Princeton, New Jersey

2. Strategies in the Design and Synthesis of Chemical Libraries

17

(22)

Eric M. Gordon, Versicor, Inc., Fremont, California

3. Solid-Phase Peptide Synthesis, Lead Generation, and Optimization

39

(72)

Bruce Seligman, SIDDCO, Tucson, Arizona

Michael Lebl, Trega Biosciences, San Diego, California

Kit S. Lam, Arizona Cancer Center, Tucson, Arizona

4. Light-Directed Chemical Synthesis of Positionally Encoded Peptide Arrays

111

(22)

Jeffrey W. Jacobs

Dinesh V. Patel

Zhengyu Yuan, Versicor, Inc., Fremont, California

Christopher P. Holmes

John Schullek, Affymax Research Institute, Palo Alto, California

Valery V. Antonenko

J. Russell Grove

Vicolay Kulikov

Derek Maclean

Marc Navre

Cindy Nguyen

Lihong Shi

Arathi Sundaram

Steven A. Sundberg, Affymax Research Institute, Santa Clara, California

5. Conformationally Restricted Peptide and Peptidomimetic Libraries

133

(18)

Alex A. Virgilio

Jonathan A. Ellman, Department of Chemistry, University of California at Berkeley, Berkeley, California

6. Submonomer Approaches for the Generation of Molecular Diversity: Nonnatural Oligomer and Organic Template Libraries

151

(14)

Lutz S. Richter

Dane A. Goff

Kerry L. Spear

Eric J. Martin

Ronald N. Zuckermann, Chiron Corporation, Emeryville, California

7. Oligonucleotide Libraries as a Source of Molecular Diversity

165

(14)

Houng-Yau Mei, Parke - Davis Pharmaceutical Research, Division of Warner - Lambert Company, Ann Arbor, Michigan

Anthony Czarnik, IRORI, La Jolla, California

PART II. Small Molecule Libraries

179

(158)

8. Small Molecule Libraries: Overview of Issues and Strategies in Library Design

181

(8)

John J. Baldwin, Pharmacopeia, Inc., Princeton, New Jersey

9. Protease Inhibitor Libraries

189

(12)

Dinesh V. Patel, Versicor, Inc., Fremont, California

David A. Campbell, Affymax Research Institute, Santa Clara, California

10. Heterocyclic Combinatorial Chemistry: Azine and Diazepine Pharmacophores

201

(12)

Mikhail F. Gordeev

Dinesh V. Patel, Versicor, Inc., Fremont, California

11. Scaffolds for Small Molecule Libraries

213

(14)

Michael R. Pavia, Millenium Pharmaceuticals Inc., Cambridge, Massachusetts

12. Application of Combinatorial Chemistry to Biopolymers

227

(16)

Edmund J. Moran, Ontogen Corp., Carlsbad, California

13. Oligosaccharide and Glycoconjugate Solid-Phase Synthesis Technologies for Drug Discovery

243

(28)

Michael J. Sofia, Transcell Technologies, Inc., Cranbury, New Jersey

14. Encoded Combinatorial Chemistry

271

(20)

Jeffrey W. Jacobs

Zhi-Jie Ni, Versicor, Inc., Fremont, California

15. Parallel Organic Synthesis in Array Format

291

(16)

Steven E. Hall, Sphinx Pharmaceuticals, A Division of Eli Lilly & Co., Durham, North Carolina

16. Synthetic Organic Chemistry on Solid Support

307

(30)

Stephen W. Kaldor

Miles G. Siegel, Lilly Research Laboratories, A Division of Eli Lilly & Company, Indianapolis, Indiana

PART III. Automation, Analytical, and Computational Methods

337

(50)

17. Automation of Combinatorial Chemistry for Large Libraries

339

(10)

Michael Needels

Jeffrey Sugarman, Affymax Research Institute, Palo Alto, California

18. Analytical Chemistry Issues in Combinatorial Organic Synthesis

349

(20)

William L. Fitch

Gary C. Look

George Detre, Affymax Research Institute, Santa Clara, California

19. Quantifying Diversity

369

(18)

Yvonne C. Martin

Robert D. Brown

Mark G. Bures, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois

PART IV. Biological Diversity

387

(32)

20. Protein Scaffolds for Peptide Libraries

389

(12)

Ronald H. Hoess, Dupont-Merck Pharmaceutical Company, Wilmington, Delaware

21. Combinatorial Biosynthesis of "Unnatural" Natural Products

401

(18)

Chaitan Khosla, Departments of Chemistry and Chemical Engineering, Stanford University, Stanford, California

PART V. Screening

419

(26)

22. Strategies for Screening Combinatorial Libraries

421

(12)

Bruce A. Beutel, Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois

23. Approaches and Technologies for Screening Large Combinatorial Libraries

433

(12)

Nolan H. Sigal

Daniel Chelsky, Pharmacopeia, Inc., Princeton, New Jersey

PART VI. Combinatorial Drug Screening and Development

445

(54)

24. Combinatorial Drug Discovery: Concepts

447

(6)

Judd Berman, Glaxo Wellcome Research Institute, Research Triangle Park, North Carolina

Russell J. Howard, Affymax Research Institute, Santa Clara, California

25. ADME/PK Assays in Screening for Orally Active Drug Candidates

453

(22)

Jacqueline A. Gibbons

Eric W. Taylor

Rene A. Braeckman, Chiron Corporation, Emeryville, California

26. Combinatorial Technologies: Prospects and Future Issues

475

(8)

James F. Kerwin, Jr., Pharmaceutical Products Division, Abbott Laboratories, Abbott Park, Illinois

27. Appendix: Combinatorial Chemistry Information Management

483

(16)

David Weininger, Daylight Chemical Information Systems, Inc., Santa Fe, New Mexico

Index

499

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Combinatorial Chemistry and Molecular Diversity in Drug Discovery

Summary

Author Biography

Table of Contents

Supplemental Materials

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Combinatorial Chemistry and Molecular Diversity in Drug Discovery

Summary

Author Biography

Table of Contents

Supplemental Materials

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