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

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

文献索引：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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被引用次数: 47

摘要

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 ...