Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5616-9. doi: 10.1016/j.bmcl.2011.06.053. Epub 2011 Jun 21.

Lipid and sulfur substituted prenylcysteine analogs as human Icmt inhibitors.

Author information

1
Department of Medicinal Chemistry and Molecular Pharmacology and Purdue University Center for Cancer Research, Purdue University, West Lafayette, IN 47907, USA.

Abstract

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.

PMID:
21782433
PMCID:
PMC4037158
DOI:
10.1016/j.bmcl.2011.06.053
[Indexed for MEDLINE]
Free PMC Article

Supplemental Content

Full text links

Icon for Elsevier Science Icon for PubMed Central
Loading ...
Support Center