Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity

…, T Galicia, C Hutchins, D Frost, SH Rosenberg…

Index: Li, Qun; Li, Tongmei; Woods, Keith W.; Gu, Wen-Zhen; Cohen, Jerry; Stoll, Vincent S.; Galicia, Tomas; Hutchins, Charles; Frost, David; Rosenberg, Saul H.; Sham, Hing L. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 11 p. 2918 - 2922

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Citation Number: 47

Abstract

A series of analogs of tipifarnib (1) has been synthesized as inhibitors of FTase by substituting the benzimidazolones and indoles for the 2-quinolone of tipifarnib. The novel benzimidazolones are potent and selective FTase inhibitors (FTIs) with IC50 values of the best compounds close to that of tipifarnib. The current series demonstrate good cellular activity as measured in their inhibiting the Ras processing in NIH-3T3 cells, with ...

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