565451-82-3Relevant academic research and scientific papers
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase
Curtin, Michael L.,Florjancic, Alan S.,Cohen, Jerome,Gu, Wen-Zhen,Frost, David J.,Muchmore, Steven W.,Sham, Hing L.
, p. 1367 - 1371 (2007/10/03)
A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (300-fold) and cellularly active (≤80 nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented.
