Potent and selective non-cysteine-containing inhibitors of protein farnesyltransferase

DJ Augeri, SJ O'Connor, D Janowick…

文献索引：Augeri, David J.; O'Connor, Stephen J.; Janowick, Dave; Szczepankiewicz, Bruce; Sullivan, Gerry; Larsen, John; Kalvin, Douglas; Cohen, Jerry; Devine, Edward; Zhang, Haichao; Cherian, Sajeev; Saeed, Badr; Ng, Shi-Chung; Rosenberg, Saul Journal of Medicinal Chemistry, 1998 , vol. 41, # 22 p. 4288 - 4300

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被引用次数: 48

摘要

Potent and selective non-thiol-containing inhibitors of protein farnesyltransferase are described. FTI-276 (1) was transformed into pyridyl ether analogue 19. The potency of pyridyl ether 19 was improved by modification of the biphenyl core to that of an o-tolyl substituted biphenyl core to give 29. In addition to 0.4 nM in vitro potency, 29 displayed 350 nM potency in whole cells as the parent carboxylic acid. The o-tolyl biphenyl core ...