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Synthesis of N,N'-disubstituted 3-aminobenzo[c] and [d]azepin-2-ones as potent and specific farnesyl transferase inhibitors
Authors:Le Diguarher Thierry  Ortuno Jean-Claude  Shanks David  Guilbaud Nicolas  Pierré Alain  Raimbaud Eric  Fauchère Jean-Luc  Hickman John A  Tucker Gordon C  Casara Patrick J
Affiliation:Department of Medicinal Chemistry, Institut de Recherches Servier, 125 chemin de Ronde, 78290 Croissy sur Seine, France.
Abstract:A structure-activity study was performed by synthesis on N,N'-disubstitution of 3-aminobenzo[c] and [d]azepin-2-one 2 and 3 to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities.
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