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

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

Bioorg Med Chem Lett

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:

Published: April 2015

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.

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http://dx.doi.org/10.1016/j.bmcl.2015.02.045DOI Listing

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