Discovery of Benzo[

Authors :: Fei, Jiang
Qinghua, Hu
Zhimin, Zhang
Hongmei, Li
Huili, Li
Dewei, Zhang
Hanwen, Li
Yu, Ma
Jingjing, Xu
Haifang, Chen
Yong, Cui
Yanle, Zhi
Yanmin, Zhang
Junyu, Xu
Jiapeng, Zhu
Tao, Lu
Yadong, Chen
Source :: Journal of medicinal chemistry. 62(24)
Publication Year :: 2019
Abstract: The bromodomain and extra-terminal domain (BET) family of proteins are readers which specifically recognize histone-acetylated lysine residues. Each BET bromodomain protein contains two highly homologous domains: the first bromodomain (BD1) and the second bromodomain (BD2). Pan-BET bromodomain inhibition is a potential therapy for various cancers and immune-inflammatory diseases, but only few reported inhibitors show selectivity within the BET family. Herein, we identified a series of benzo[

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