1. Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives
- Author
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Fanny Roussi, Fabio La Spisa, Maria Concepcion Garcia Alvarez, Olga Gherbovet, Jérôme Bignon, Hélène Levaique, Sylviane Thoret, Institut de Chimie des Substances Naturelles (ICSN), Centre National de la Recherche Scientifique (CNRS)-Institut de Chimie du CNRS (INC), Dipartimento di Scienze del Farmaco, and Università degli Studi del Piemonte Orientale - Amedeo Avogadro (UPO)
- Subjects
Vinca ,Stereochemistry ,Clinical Biochemistry ,Pharmaceutical Science ,Antineoplastic Agents ,Vinblastine ,Biochemistry ,Tubulin ,Cell Line, Tumor ,Drug Discovery ,[CHIM]Chemical Sciences ,Humans ,Molecular Biology ,Vinca Alkaloids ,ComputingMilieux_MISCELLANEOUS ,Biological evaluation ,Cell Proliferation ,Anhydrovinblastine ,biology ,Chemistry ,Organic Chemistry ,Vinorelbine ,biology.organism_classification ,HCT116 Cells ,Tubulin Modulators ,3. Good health ,Molecular Medicine ,K562 Cells - Abstract
Recent publications highlighted that vinca derivatives either functionalized on C-12′ or enlarged on cycle C′ could be more cytotoxic than vinblastine or vinorelbine, both used in anti-cancer therapy. By combining these two results, nine new 7′- homo -anhydrovinblastine derivatives functionalized on C-13′ were elaborated. The synthesis of key intermediates, their one-step transformation into final products in mild conditions and their biological activities are presented
- Published
- 2014
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