Design, synthesis and biological evaluation of benzo[cd]indol-2(1H)-ones derivatives as BRD4 inhibitors.

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作者： Yuxin,Feng ^[1] ; Senhao,Xiao ^[2] ; Yantao,Chen ^[3] ; Hao,Jiang ^[3] ; Na,Liu ^[1] ; Cheng,Luo ^[3] ; Shijie,Chen ^[4] ; Hua,Chen ^[5]

作者单位： Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding, 071002, China. ^[1] Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, Shanghai, 201203, China; University of Chinese Academy of Sciences, Beijing, 100049, China; School of Life Science and Technology, Shanghai Tech University, Shanghai, 200031, China. ^[2] Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, Shanghai, 201203, China; University of Chinese Academy of Sciences, Beijing, 100049, China. ^[3] Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of MateriaMedica, Chinese Academy of Sciences, Shanghai, 201203, China; University of Chinese Academy of Sciences, Beijing, 100049, China. Electronic address: shijiechen@simm.ac.cn. ^[4] Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding, 071002, China. Electronic address: hua-todd@163.com. ^[5]

关键词 Acetyl-lysine binding pocket BRD4 inhibitor Benzo[cd]indol-2(1H)-one Bromodomain and extra-terminal domain Sulfonamide