Non-Thiol Farnesyltransferase Inhibitors: Structure-Activity Relationships of Aralkylsubsituted Benzophenones
- 1 February 2001
- journal article
- research article
- Published by Wiley in Archiv der Pharmazie
- Vol. 334 (2) , 40-44
- https://doi.org/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).Keywords
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