852510-51-1Relevant articles and documents
Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors
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.
, p. 2033 - 2039 (2007/10/03)
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 against FTase than tipifarnib.
