图书简介
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
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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