The Ups and Downs in Drug Design: Adventures in Medicinal Chemistry

ISBN-13: 9781032067100 / Angielski / Twarda / 2021 / 452 str.

Victor Marquez

Opis

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.

Spis treści

1. STRUCTURE-ACTIVITY RELATIONSHIPS (SAR). 2. BRAIN ANTITUMOR AGENTS: THE STORY OF SPIROMUSTIN. 3. PRIVILEGED DRUG SCAFFOLDS: THE STORY OF LC-6 AND PYRIDINOLCARBAMATE. 4. CYTIDINE DEAMINASE: PART 1—THE CONCEPT OF TRANSITION-STATE INHIBITORS AND THE DISCOVERY OF ZEBULARINE. 5. CYTIDINE DEAMINASE: PART 2—LESSONS FROM NATURE’S TRANSITION STATE INHIBITORS. 6. TIAZOFURIN AND THE HISTORY OF THIAZOLE-4-CARBOXAMIDE ADENIDE DINUCLEOTIDE (TAD). 7. THE AIDS ERA: NUCLEOSIDE ANTIRETROVIRAL AGENTS. 8. THE AIDS ERA: SYNTHESES OF FLUORONUCLEOSIDES AND THE CLINICAL DEVELOPMENT OF LODENOSINE. 9. EXPLORATION OF NOVEL NUCLEOSIDE TEMPLATES IN SEARCH OF ACTIVE ANTI-HIV AND ANTIVIRAL DRUGS. 10. 3-DEAZANEPLANOCIN A AND CYCLOPENTENYLCYTOSINE. 11. EPIGENETICS AND CANCER: 5-AZA-CYTIDINE AND ZEBULARINE. 12. ZEBULARINE AS AN EPIGENETIC ANTICANCER AGENT. 13. 3-DEAZANEPLANOCIN A (DZNep) AS AN EPIGENETIC ANTICANCER AGENT. 14. BICYCLO[3.1.0]HEXANE NUCLEOSIDES: CHEMISTRY.  15. BICYCLO[3.1.0]HEXANE NUCLEOSIDES: BIOLOGY (PART 1). 16. BICYCLO[3.1.0]HEXANE NUCLEOSIDES: BIOLOGY (PART 2)—MORE ON KINASES/POLYMERASES AND DRUG DEVELOPMENT OF N-MCT. 17. BICYCLO[3.1.0]HEXANE NUCLEOSIDES: BIOLOGY (PART THREE)—INVESTIGATION OF MORE EXOTIC TARGETS. 18. BICYCLO[3.1.0]HEXANE NUCLEOSIDES: CHEMICAL VARIATIONS ON A COMMON THEME. 19. DIACYLGLYCEROL LACTONES AND PROTEIN KINASE C (PKC): A PHARMACOPHORE-GUIDED APPROACH. 20. DIACYLGLYCEROL LACTONES AND PROTEIN KINASE C (PKC): TRANSITION FROM A PHARMACOPHORE-GUIDED APPROACH TO A RECEPTOR-GUIDED APPROACH.

O autorze

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.