Title of article
Potent inhibitors of farnesyltransferase and geranylgeranyltransferase-I
Author/Authors
Diem N. Nguyen، نويسنده , , Craig A. Stump، نويسنده , , Eileen S. Walsh، نويسنده , , Christine Fernandes، نويسنده , , Joseph P. Davide، نويسنده , , Michelle Ellis-Hutchings، نويسنده , , Ronald G. Robinson، نويسنده , , Theresa M. Williams، نويسنده , , Robert B. Lobell، نويسنده , , Hans E. Huber، نويسنده , , Carolyn A. Buser، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2002
Pages
5
From page
1269
To page
1273
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2002
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
792193
Link To Document