2. Academic Validation
  3. Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives

Synthesis and biological evaluation of C-13' substituted 7'-homo-anhydrovinblastine derivatives

  • Bioorg Med Chem Lett. 2015 Apr 15;25(8):1771-1773. doi: 10.1016/j.bmcl.2015.02.045.
Olga Gherbovet 1,  Fabio La Spisa 2,  Sylviane Thoret 1,  Maria Concepcion Garcia Alvarez 1,  Hélène Levaique 1,  Jérôme Bignon 1,  Fanny Roussi 3
Affiliations

Affiliations

  • 1 Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, UPR 2301 du CNRS, Avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France.
  • 2 Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale 'A. Avogadro', Largo Donegani 2, 28100 Novara, Italy.
  • 3 Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, UPR 2301 du CNRS, Avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France. Electronic address: fanny.roussi@cnrs.fr.
PMID: 25804719 DOI: 10.1016/j.bmcl.2015.02.045
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.

Keywords

7′-homo-Anhydrovinblastine; Cancer; Cytotoxicity; Tubulin; Vinca alkaloids.

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