Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors |
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Authors: | 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 |
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Affiliation: | Cancer Research, GPRD, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. qun.li@abbott.com |
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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 against FTase than tipifarnib. |
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