Non-thiol farnesyltransferase inhibitors: structure-activity relationships of aralkylsubstituted benzophenones.
作者信息
Mitsch A, Wissner P, Sattler I, Schlitzer M
机构信息
Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, D-35032 Marburg, Germany.
出版信息
Arch Pharm (Weinheim). 2001 Feb;334(2):40-4. doi: 10.1002/1521-4184(200102)334:2<40::aid-ardp40>3.0.co;2-w.
Abstract
We describe a novel class of benzophenone-based farnesyltransferase inhibitors exploiting a novel aryl binding region in the farnesyltransferase's active site. The present study was mainly focussed on structural modifications of the trimethylene spacer of the 4-phenyl butyroyl residue of our lead structure (IC50 = 530 nM). These modifications turned out to have little effect on activity as had the replacement of the terminal aryl by cyclohexyl (IC50 = 440 nM vs. IC50 = 530 nM).
摘要
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