312936-83-7Relevant academic research and scientific papers
Synthesis of a14C-labeled FPTase inhibitor via a Pd-catalyzed cyanation with Zn(14CN)2 and via bromo[ 14C]acetic acid
Ho, Jonathan Z.,Elmore, Charles S.,Braun, Matthew P.
experimental part, p. 399 - 403 (2009/04/07)
14C-Labeled farnesyl-protein transferase inhibitor 1a was required for drug metabolism studies. The first approach was to synthesize 14C-labeled 1b using Zn(14CN)2 in a Pd-catalyzed cyanation. A second approach was to prepare labeled 1c with the 14C-label in the piperazine ring. All metabolites from 1b were non-radioactive whereas the same metabolites from 1c were all radioactive and quantifiable. Copyright
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.
