Discovery of thioazepinone ligands for Src SH2: From non-specific to specific binding

被引：20

作者：

Lesuisse, D

Deprez, P

Albert, E

Duc, TT

Sortais, B

Gofflo, D

Jean-Baptiste, V

Marquette, JP

Schoot, B

Sarubbi, E

Lange, G

Broto, P

Mandine, E

机构：

[1] Aventis, Dept Med Chem, F-93235 Romainville, France

[2] Aventis, Bone Dis Grp, F-93235 Romainville, France

[3] Aventis, Core Res, F-93235 Romainville, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(01)00386-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：2127 / 2131

页数：5

共 17 条

[1] L-ALPHA-AMINO-BETA-THIO-EPSILON-CAPROLACTAM, A NEW SULFUR-CONTAINING SUBSTRATE FOR ALPHA-AMINO-EPSILON-CAPROLACTAM RACEMASE [J].