作者:B.Wesley Trotter、Amy G. Quigley、William C. Lumma、John T. Sisko、Eileen S. Walsh、Christian S. Hamann、Ronald G. Robinson、Hema Bhimnathwala、D.Garrett Kolodin、Wei Zheng、Carolyn A. Buser、Hans E. Huber、Robert B. Lobell、Nancy E. Kohl、Theresa M. Williams、Samuel L. Graham、Christopher J. Dinsmore
DOI:10.1016/s0960-894x(01)00061-0
日期:2001.4
A series of 2-arylindole-3-acetamide farnesylproteintransferaseinhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesylproteintransferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation