| Description |
1 online resource (475 p.) |
| Contents |
Cover -- Half Title -- Title -- Copyright -- Contents -- Foreword -- Acknowledgments -- Author -- Introduction -- 1. Structure-Activity Relationships (SAR) -- 1.1 Undergraduate Academic Training (1961-1966), School of Pharmacy, Central University of Venezuela -- 1.2 Graduate Studies in Medicinal Chemistry (1966-1970) at the University of Michigan, Ann Arbor, Michigan -- 1.2.1 Antimalarial Agents -- 1.2.2 The Mechanism of Action of Amodiaquine -- 1.2.3 The Mechanism of Action of Chloroquine -- 1.3 Biogenic 4-Hydroxytryptamines: Approaches to the Synthesis of Baeocystin -- 1.4 Conclusions |
|
2. Brain Antitumor Agents: The Story of Spiromustin -- 2.1 Postdoctoral Fellowship (September 1970-September 1971) at the Drug Development Branch, National Cancer Institute, National Institutes of Health (NIH), Bethesda, Maryland -- 2.2 Central Nervous System Antitumor Agents, Nitrogen Mustards, and the Concept of Partition Coefficient -- 2.3 Exploring New Chemistry -- 2.4 Conclusions -- 3. Privileged Drug Scaffolds: The Story of LC-6 and Pyridinolcarbamate -- 3.1 Research Director, Laboratorios Cosmos, S. A., Caracas, Venezuela (January 1972-April 1977) -- 3.2 Head of a Mouse or Tail of a Lion |
|
3.3 Where to Start? -- 3.4 Nitrogen-Containing Steroidal Analogues (Aza-Steroids) -- 3.5 The Biological Activity of LC-6 -- 3.6 Pyridinol Carbamate Analogues -- 3.7 Additional Studies -- 3.8 Conclusions -- 4. Cytidine Deaminase: Part 1-The Concept of Transition-State Inhibitors and the Discovery of Zebularine -- 4.1 Laboratory of Pharmacology and Experimental Therapeutics, Medicinal Chemistry Section, National Cancer Institute, Bethesda, Maryland -- 4.2 A Brief Primer on Nucleosides and Nucleotides -- 4.3 Transition-State Inhibitors and Cytidine Deaminase -- 4.4 Tetrahydrouridine (THU) |
|
4.5 Zebularine -- 4.6 Proof of Concept -- 4.7 Metabolism of Zebularine and dCMP Deaminase -- 4.8 Incorporation of Zebularine into DNA -- 4.9 Zebularine Analogues -- 4.10 Conclusions -- 5. Cytidine Deaminase: Part 2-Lessons from Nature's Transition-State Inhibitors -- 5.1 Two Important Aminohydrolases (CDA and ADA) -- 5.2 Seven-Membered 1,3-Diazepinone Nucleosides -- 5.3 Variation on the 1,3-Diazepinone Theme -- 5.4 The Search of a General Synthetic Method to Make 1,3-Diazepin-2-One Nucleobases |
|
5.5 The Selection of Reactive Sugar Precursors and Catalysts for the Successful Coupling of 1,3-Diazepin-2-One Nucleobases -- 5.6 Development of Methods for Adding Additional Functionality to Already Coupled 1,3-Diazepin-2-One Nucleosides -- 5.7 How Important Is Ring Size? -- 5.8 Proof of Concept -- 5.9 Alternative Approaches to Nucleosides with Seven-Membered Rings and the Magic of Zebularine Chemistry -- 5.10 Conclusions -- 6. Tiazofurin and the History of Thiazole-4-Carboxamide Adenide Dinucleotide (TAD) |
| Notes |
Description based upon print version of record |
|
6.1 National Cancer Institute, Laboratory of Medicinal Chemistry and Biology, NIH, Bethesda, Maryland |
| Form |
Electronic book
|
| ISBN |
9781000462944 |
|
1000462943 |
|
