Second-generation peptidomimetic inhibitors of protein farnesyltransferase demonstrating improved cellular potency and significant in vivo efficacy

…, J Cohen, E Devine, S Cherian, B Saeed…

Index: O'Connor, Stephen J.; Barr, Kenneth J.; Wang, Le; Sorensen, Bryan K.; Tasker, Andrew S.; Sham, Hing; Shi-Chung, Ng; Cohen, Jerome; Devine, Edward; Cherian, Sajeev; Saeed, Badr; Zhang, Haichao; Jang Yun, Lee; Warner, Robert; Tahir, Stephen; Kovar, Peter; Ewing, Patricia; Alder, Jeffrey; Mitten, Michael; Leal, Juan; Marsh, Kennan; Bauch, Joy; Hoffman, Daniel J.; Sebti, Said M.; Rosenberg, Saul H. Journal of Medicinal Chemistry, 1999 , vol. 42, # 18 p. 3701 - 3710

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Citation Number: 40

Abstract

The synthesis and evaluation of analogues of previously reported farnesyltransferase inhibitors, pyridyl benzyl ether 3 and pyridylbenzylamine 4, are described. Substitution of 3 at the 5-position of the core aryl ring resulted in inhibitors of equal or less potency against the enzyme and decreased efficacy in a cellular assay against Ras processing by the enzyme. Substitution of 4 at the benzyl nitrogen yielded 26, which showed improved ...

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