Dipartimento di Chimica e Tecnologie del Farmaco, Istituto Pasteur-Fondazione Cenci Bolognetti, Sapienza Università di Roma , Piazzale Aldo Moro 5, I-00185 Roma, Italy.
J Med Chem. 2013 Feb 14;56(3):625-7. doi: 10.1021/jm400002j. Epub 2013 Jan 14.
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.
Boger 等人合成了一系列长春碱的 C20' 脲衍生物,这些衍生物在细胞生长抑制试验中与长春碱的活性相当或超过了长春碱的活性。这些研究表明 C20' 位上氢键供体的重要性,并揭示了 C20' 取代基周围存在一个空间,可以容纳各种取代基,显著提高了长春碱类似物的活性。