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

P Gilleron, N Wlodarczyk, R Houssin, A Farce…

Index: Gilleron, Pauline; Wlodarczyk, Nicolas; Houssin, Raymond; Farce, Amaury; Laconde, Guillaume; Goossens, Jean-Francois; Lemoine, Amelie; Pommery, Nicole; Henichart, Jean-Pierre; Millet, Regis Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 19 p. 5465 - 5471

Full Text: HTML

Citation Number: 23

Abstract

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.