Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors |
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Authors: | Li Qun Claiborne Akiyo Li Tongmei Hasvold Lisa Stoll Vincent S Muchmore Steven Jakob Clarissa G Gu Wendy Cohen Jerry 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: | As a part of our efforts to identify potent inhibitors of farnesyltransferase (FTase), modification of the structure of tipifarnib through structure-based design was undertaken by replacing the 2-quinolones with 4-quinolones and pyridones, and subsequent relocation of the D-ring to the N-methyl group on the imidazole ring. This study has yielded a novel series of potent and selective FTase inhibitors. The X-ray structure of tipifarnib (1) in complex with FTase was described. |
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