Parallel liquid synthesis of N, N′-Disubstituted 3-amino azepin-2-ones as potent and specific farnesyl transferase inhibitors

T Le Diguarher, JC Ortuno, G Dorey, D Shanks…

文献索引：Le Diguarher, Thierry; Ortuno, Jean-Claude; Dorey, Gilbert; Shanks, David; Guilbaud, Nicolas; Pierre, Alain; Fauchere, Jean-Luc; Hickman, John A.; Tucker, Gordon C.; Casara, Patrick J. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 14 p. 3193 - 3204

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被引用次数: 12

摘要

A rapid structure–activity study was performed by parallel liquid synthesis on N, N′- disubstitution of 3-amino azepin-2-one to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities. The activities of the selected compounds were validated in vivo, and compounds 41a and 44a presented significant antitumour activity.

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