Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors

ArticleinBioorganic & medicinal chemistry letters 19(6):1753-7 · March 2009with9 Reads
Impact Factor: 2.42 · DOI: 10.1016/j.bmcl.2009.01.074 · Source: PubMed


    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.