Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 18, Pages 5616-5619Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.053
Keywords
Isoprenylcysteine carboxylmethyltransferase; Amino acid analogs; Enzyme inhibitors; Isoprenoids; Click chemistry
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Funding
- NIH [R01 CA112483, P30 CA21328]
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Inhibition of isoprenylcysteine carboxyl methyltransferase (Icmt) offers a promising strategy for K-Ras driven cancers. We describe the synthesis and inhibitory activity of substrate-based analogs derived from several novel scaffolds. Modifications of both the prenyl group and thioether of N-acetyl-S-farnesyl-L-cysteine (AFC), a substrate for human Icmt (hIcmt), have resulted in low micromolar inhibitors of Icmt and have given insights into the nature of the prenyl binding site of hIcmt. (C) 2011 Elsevier Ltd. All rights reserved.
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