New prospects for vinblastine analogues as anticancer agents.

Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza Università di Roma , Piazzale Aldo Moro 5, I-00185 Roma, Italy. romano.silvestri@uniroma1.it

Journal of medicinal chemistry 2013 Feb 14

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Boger et al. synthesized a series of C20' urea derivatives of vinblastine that matched or exceeded the potency of vinblastine in cell growth inhibition assays. The studies demonstrated the importance of the H-bond donor on the C20' position and revealed the presence of a space surrounding the C20' substituent that tolerates a wide variety of substituents, remarkably enhancing potency of vinblastine analogues.