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

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  = 1.1 nM) and antitumor activity in human cancer xenografts in mice.