Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I

…, M Ellis-Hutchings, RG Robinson, TM Williams…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 9 p. 1269 - 1273

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Citation Number: 20

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.