ABSTRACT

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

chapter 1|10 pages

Structure-Activity Relationships (SAR)

chapter 2|6 pages

Brain Antitumor Agents

The Story of Spiromustin

chapter 3|10 pages

Privileged Drug Scaffolds

The Story of LC-6 and Pyridinolcarbamate

chapter 4|10 pages

Cytidine Deaminase

Part 1—The Concept of Transition-State Inhibitors and the Discovery of Zebularine

chapter 5|14 pages

Cytidine Deaminase

Part 2—Lessons from Nature's Transition-State Inhibitors

chapter 7|26 pages

The AIDS Era

Nucleoside Antiretroviral Agents

chapter 8|14 pages

The AIDS Era

Syntheses of Fluoronucleosides and the Clinical Development of Lodenosine

chapter 11|22 pages

Epigenetics and Cancer

5-Aza-Cytidine and Zebularine

chapter 12|20 pages

Zebularine as an Epigenetic Anticancer Agent

chapter 14|26 pages

Bicyclo[3.1.0]Hexane Nucleosides

Chemistry

chapter 15|36 pages

Bicyclo[3.1.0]Hexane Nucleosides

Biology (Part 1)

chapter 16|24 pages

Bicyclo[3.1.0]Hexane Nucleosides

Biology (Part 2)—More on Kinases/Polymerases and Drug Development of N-MCT

chapter 17|24 pages

Bicyclo[3.1.0]Hexane Nucleosides

Biology (Part 3)—Investigation of More Exotic Targets

chapter 18|28 pages

Bicyclo[3.1.0]Hexane Nucleosides

Chemical Variations on a Common Theme

chapter 19|30 pages

Diacylglycerol Lactones and Protein Kinase C (PKC)

A Pharmacophore-Guided Approach

chapter 20|34 pages

Diacylglycerol Lactones and Protein Kinase C (PKC)

Transition from a Pharmacophore-Guided Approach to a Receptor-Guided Approach