The Ups and Downs in Drug Design : Adventures in Medicinal Chemistry book cover
1st Edition

The Ups and Downs in Drug Design
Adventures in Medicinal Chemistry





ISBN 9781032063638
Published November 16, 2021 by CRC Press
474 Pages 76 Color & 403 B/W Illustrations

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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 author’s own personal experience in this field and describes the "ups" and "downs" that come with drug discovery. It 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

  • Illustrates "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 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 After one year of postdoctoral studies at the National Cancer Institute (NCI)/National Institutes of Health (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 he was Chief of the Laboratory of Medicinal Chemistry. 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 retired as Scientist Emeritus after 32 years of service.

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

 

The purpose of this book is to describe Dr. Marquez's journey/career in medicinal chemistry in a semi-autobiographical function. As it follows his own personal journey, the "chapters" seem random as they parallel his career path and the work/molecules he studied. It is a rather unique text as a career "summary" for Dr. Marquez.

In my opinion as a pharmacy educator, the target audience of this book is primarily colleague medicinal chemists who can relate to the changes in the field over the past four decades. Graduate-level students in this field also may admire the pathway and trials and tribulations of a mentoring medicinal chemist. Based on his longstanding career, Dr. Marquez is a leader in this field and an educator.

This is the first book of this style I have come across in my academic career. As the book is based on Dr. Marquez' personal journal, it is rather unique, but a second edition will not apply.

- Patrick J. McDonnell, PharmD (Temple University School of Pharmacy)