Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3, 4, 5-trimethoxybenzoyl) benzo [b] furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and …

…, TC Lavranos, DK Chalmers, SA Charman…

文献索引：Flynn, Bernard L.; Gill, Gurmit S.; Grobelny, Damian W.; Chaplin, Jason H.; Paul, Dharam; Leske, Annabell F.; Lavranos, Tina C.; Chalmers, David K.; Charman, Susan A.; Kostewicz, Edmund; Shackleford, David M.; Morizzi, Julia; Hamel, Ernest; Jung, M. Katherine; Kremmidiotis, Gabriel Journal of Medicinal Chemistry, 2011 , vol. 54, # 17 p. 6014 - 6027

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被引用次数: 77

摘要

A structure–activity relationship (SAR) guided design of novel tubulin polymerization inhibitors has resulted in a series of benzo [b] furans with exceptional potency toward cancer cells and activated endothelial cells. The potency of early lead compounds has been substantially improved through the synergistic effect of introducing a conformational bias and additional hydrogen bond donor to the pharmacophore. Screening of a focused ...