Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors

…, W Wang, NH Lin, A Claiborne, W Gu, J Cohen…

Index: Li, Qun; Woods, Keith W.; Wang, Weibo; Lin, Nan-Horng; Claiborne, Akiyo; Gu, Wen-Zhen; Cohen, Jerry; Stoll, Vincent S.; Hutchins, Charles; Frost, David; Rosenberg, Saul H.; Sham, Hing L. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 8 p. 2033 - 2039

Full Text: HTML

Citation Number: 29

Abstract

Beginning with the structure of tipifarnib (1), a series of inhibitors of FTase have been synthesized by transposition of the D-ring to the imidazole and subsequent modification of the 2-quinolone motif. The compounds in the new series may be achiral and have structural features that allow for analogs that are difficult or impossible to make in the tertiary carbon- based tipifarnib series. The most potent compound (4d) is 4 times more active in vitro ...