Small-molecule inhibitors of the cancer target, isoprenylcysteine carboxyl methyltransferase, from Hovea parvicalyx.

Abstract

Isoprenylcysteine carboxyl methyltransferase (Icmt) is enzyme target in anticancer drug discovery. An Icmt natural product high-throughput screening campaign was conducted and a hit extract from the roots of Hovea parvicalyx was identified. 2'-Methoxy-3'-prenyl-licodione and 2'-methoxy-3',3''-diprenyl-licodione, two prenylated beta-hydroxychalcone compounds, together with the known flavanone (S)-glabrol, were isolated and identified as bioactive constituents. Their structures were determined largely by 1D and 2D NMR spectroscopy.

• Authors: Malcolm S Buchanan, Anthony R Carroll, Gregory A Fechner, Anthony Boyle, Moana Simpson, Rama Addepalli, Vicky M Avery, Paul I Forster, Gordon P Guymer, Tony Cheung, Huwei Chen, Ronald J Quinn
• Journal: Phytochemistry (Phytochemistry) Vol. 69 Issue 9 Pg. 1886-9 (Jun 2008) ISSN: 0031-9422 [Print] England
• PMID: 18466935 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Enzyme Inhibitors
• Protein Methyltransferases
• protein-S-isoprenylcysteine O-methyltransferase

Topics

• Antineoplastic Agents (chemistry)
• Enzyme Inhibitors (chemistry)
• Fabaceae (chemistry)
• Magnetic Resonance Spectroscopy
• Molecular Structure
• Protein Methyltransferases (antagonists & inhibitors, metabolism)