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…

Index: 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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Citation Number: 12

Abstract

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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