1st Edition

The Ups and Downs in Drug Design
Adventures in Medicinal Chemistry




  • Available for pre-order. Item will ship after November 2, 2021
ISBN 9781032063638
November 2, 2021 Forthcoming by CRC Press
464 Pages 76 Color & 403 B/W Illustrations

USD $130.00

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Book Description

The Ups and Downs in Drug Design: Adventures in Medicinal Chemistry highlights the necessity for an integrative approach in Medicinal Chemistry and Chemical Biology. As Medicinal Chemistry is not a monolithic science, it is important to emphasize the other various disciplines that are required for successful drug design. This book presents the authors' own personal experience in this field and describes the "ups" and "downs" that come with drug discovery. This book is an excellent companion text for graduate and postgraduate students who would like further insight into the parameters of drug design, including the challenges that come with the project.

Key Features:

  • Describes 'real life' examples in Medicinal Chemistry. Integrates the use of physical, chemical, and biological concepts that are important in drug design.
  • Highlights the "ups" and "downs" that come with drug discovery.
  • Aims to inspire students who may be struggling with the challenges and thought process in drug design.
  • Intends to be an excellent companion text, illustrating real life experiences, for graduate and postgraduate students.

Table of Contents

Acknowledgements

About the Author

Foreword

Introduction 

Chapter 1. STRUCTURE-ACTIVITY-RELATIONSHIPS (SAR)

Chapter 2. BRAIN ANTI-TUMOR AGENTS. THE STORY OF SPIROMUSTIN 

Chapter 3. PRIVILEGED DRUG SCAFFOLDS. THE STORY OF LC-6 AND PYRIDINOLCARBAMATE.

Chapter 4. CYTIDINE DEAMINASE PART 1.  THE CONCEPT OF TRANSITION-STATE INHIBITORS AND THE DISCOVERY OF ZEBULARINE.

Chapter 5. CYTIDINE DEAMINASE PART 2. LESSONS FROM NATURE’S TRANSITION STATE INHIBITORS.

Chapter 6. TIAZOFURIN AND THE HISTORY OF THIAZOLE-4-CARBOXAMIDE ADENIDE DINUCLEOTIDE (TAD).

Chapter 7. THE AIDS ERA: NUCLEOSIDE ANTIRETROVIRAL AGENTS.

Chapter 8. THE AIDS ERA: SYNTHESES OF FLUORONUCLEOSIDES AND THE CLINICAL DEVELOPMENT OF LODENOSINE.

Chapter 9. EXPLORATION OF NOVEL NUCLEOSIDE TEMPLATES IN SEARCH OF ACTIVE ANTI-HIV AND ANTIVIRAL DRUGS.

Chapter 10.  3-DEAZANEPLANOCIN A AND CYCLOPENTENYLCYTOSINE. 

Chapter 11. EPIGENETICS AND CANCER: 5-AZA-CYTIDINE AND ZEBULARINE. 

Chapter 12. ZEBULARINE AS AN EPIGENETIC ANTICANCER AGENT.

Chapter 13. 3-DEAZANEPLANOCIN A (DZNep) AS AN EPIGENETIC ANTICANCER AGENT.

Chapter 14. BICYCLO[3.1.0]HEXANE NUCLEOSIDES. CHEMISTRY.

Chapter 15. BICYCLO[3.1.0]HEXANE NUCLEOSIDES. BIOLOGY (PART ONE).

Chapter 16. BICYCLO[3.1.0]HEXANE NUCLEOSIDES. BIOLOGY (PART TWO). MORE ON KINASES/POLYMERASES AND DRUG DEVELOPMENT OF N-MCT.

Chapter 17. BICYCLO[3.1.0]HEXANE NUCLEOSIDES. BIOLOGY (PART THREE). INVESTIGATING OF MORE EXOTIC TARGETS.

Chapter 18. BICYCLO[3.1.0]HEXANE NUCLEOSIDES. CHEMICAL VARIATIONS ON A COMMON THEME.

Chapter 19. DIACYLGLYCEROL LACTONES AND PROTEIN KINASE C (PKC). A PHARMACOPHORE-GUIDED APPROACH.

Chapter 20. DIACYLGLYCEROL LACTONES AND PROTEIN KINASE C (PKC). TRANSITION FROM A PHARMACOPHORE GUIDED APPROACH TO A RECEPTOR GUIDED APPROACH.

References

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Author(s)

Biography

Dr. Victor E. Marquez was born in Venezuela in 1943 and became a naturalized US citizen in 1989. Graduated with a BS degree in Pharmacy from the Central University of Venezuela (1966) and received MS (1968) and Ph.D. (1970) degrees in Medicinal Chemistry from the University of Michigan. After one-year of postdoctoral studies at the NCI/NIH, Dr. Marquez returned to Venezuela as Research Director of Cosmos Laboratories. In 1977, he rejoined the NCI as a Visiting Scientist, and from 1999 to 2009 became Chief of the Laboratory of Medicinal Chemistry. Dr. Marquez retired as Scientist Emeritus after 32 years of service and during his career he authored or co-authored 408 research publications. In 2008 Dr. Marquez was named Maryland Chemist of the year and in 2010 he was inducted into the Medicinal Chemistry Hall of Fame. Dr. Marquez is married to Beatriz Castillo de Marquez, former Engineering student at the University of Michigan. They have four children, Victor Henrique, Gonzalo Alberto, Adriana Maria, and Daniela Virginia, three of them University of Michigan alumni.

Reviews

In this book, Dr. Marquez goes to great lengths to explain the chemical rationales that he and his teams followed including the development and utilization of efficient synthetic schemes and the molecular mechanisms of action of the potential drug candidates that they pursued.  The stories that Dr. Marquez relates illustrate the challenges they faced, the joys of the successes and the frustrations of the defeats in drug discovery.  More importantly, they guide the reader through the thought processes and what was learned in each of these efforts even when the success was less than hoped for.  This book is a wonderful lesson for those bright young minds who are considering careers in the biomedical sciences as well as those already on the pathway and indeed experienced practitioners too.

- George A. Garcia, from the Foreword