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Discovery of thioazepinone ligands for Src SH2: from non-specific to specific binding
D Lesuisse1, P Deprez, E Albert
1Department of Medicinal Chemistry, Aventis, 102 route de Noisy, 93235 Romainville Cedex, France. dominique.lesuisse@aventis.com
Bioorganic & Medicinal Chemistry Letters
|August 22, 2001
Abstract:
The structure-based design and synthesis of new thioazepinones as ligands for Src SH2 protein is presented. From benzothioazepinones, ligands with somewhat unspecific binding properties, simpler thioazepinones were designed, the best ones demonstrated nanomolar affinity for Src SH2. A few of these new ligands were crystallized with the protein and demonstrated a specific binding mode with the protein.