Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors

A new series of FTase inhibitors containing a tricyclic moiety—dioxodibenzothiazepine or dibenzocycloheptane—has been designed and synthesized. Among them, dioxodibenzothiazepine 18d displayed significant inhibitory FTase activity (IC50 = 17.3 nM) and antiproliferative properties.

The design, synthesis, inhibitory FTase activity and antiproliferative properties of the title tricyclic compounds are reported.Figure optionsDownload as PowerPoint slide