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Bioorg Med Chem Lett. 2002 May 6;12(9):1269-73.

Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. diem_nguyen@merck.com

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.

PMID:
11965368
DOI:
10.1016/s0960-894x(02)00154-3
[Indexed for MEDLINE]

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