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Discovery of Benzo[d]imidazole-6-sulfonamides as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the First Bromodomain
ChemMedChem ( IF 3.4 ) Pub Date : 2022-08-30 , DOI: 10.1002/cmdc.202200343
Alessandra Cipriano 1 , Ciro Milite 1 , Alessandra Feoli 1 , Monica Viviano 1 , Giacomo Pepe 1 , Pietro Campiglia 1 , Giuliana Sarno 1 , Sarah Picaud 2 , Satomi Imaide 3, 4 , Nikolai Makukhin 3, 5 , Panagis Filippakopoulos 2 , Alessio Ciulli 3 , Sabrina Castellano 1 , Gianluca Sbardella 1
Affiliation  

Bioisosteric replacement of the azobenzene moiety of selective BET inhibitors with a benzimidazole ring afforded a set of benzimidazole-6-sulfonamides. Evaluation of the binding activity against diverse BRD families endorses the benzimidazole as a useful scaffold to obtain compounds with improved selectivity towards the first bromodomains of BET family proteins.

中文翻译:

发现苯并 [d] 咪唑-6-磺胺作为 Bromodomain 和额外终端域 (BET) 抑制剂,对第一个 Bromodomain 具有选择性

用苯并咪唑环生物等排取代选择性 BET 抑制剂的偶氮苯部分,得到一组苯并咪唑-6-磺酰胺。对不同 BRD 家族的结合活性的评估支持苯并咪唑作为一种有用的支架,以获得对 BET 家族蛋白的第一个溴结构域具有更高选择性的化合物。
更新日期:2022-08-30
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