| Literature DB >> 11965368 |
Diem N Nguyen1, Craig A Stump, Eileen S Walsh, Christine Fernandes, Joseph P Davide, Michelle Ellis-Hutchings, Ronald G Robinson, Theresa M Williams, Robert B Lobell, Hans E Huber, Carolyn A Buser.
Abstract
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.Mesh：
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Year: 2002 PMID： 11965368 DOI： 10.1016/s0960-894x(02)00154-3
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823