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

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