254108-76-4Relevant academic research and scientific papers
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I
Nguyen, Diem N.,Stump, Craig A.,Walsh, Eileen S.,Fernandes, Christine,Davide, Joseph P.,Ellis-Hutchings, Michelle,Robinson, Ronald G.,Williams, Theresa M.,Lobell, Robert B.,Huber, Hans E.,Buser, Carolyn A.
, p. 1269 - 1273 (2007/10/03)
Compound 1 has been shown to be a dual prenylation inhibitor with FPTase (IC50=2 nM) and GGPTase-I (IC50=95 nM). Analogues of 1, which replaced the cyanophenyl group with various biaryls, led to the discovery of highly potent dual FPTase/GGPTase-I inhibitors. 4-Trifluoromethylphenyl, trifluoropentynyl, and trifluoropentyl were identified as good p-cyano replacements.
