Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.

Kamakura Research Laboratories, Chugai Pharmaceutical Co. Ltd., 200-Kajiwara, Kamakura, Kanagawa 247-8530, Japan.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.65). 03/2009; 19(6):1753-7. DOI:10.1016/j.bmcl.2009.01.074
Source: PubMed

ABSTRACT A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice.

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Kohsuke Asoh