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1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors. 2014
Lixin Wu, and
Meiqi Lu, and
Zhihui Yan, and
Xiaobin Tang, and
Bo Sun, and
Wei Liu, and
Honggang Zhou, and
Cheng Yang
College of Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, China.
A novel series of 1,2-benzisothiazol-3-one derivatives was synthesized and their biological activities were evaluated for inhibiting caspase-3 and -7 activities, in which some of them showed low nanomolar potency against caspase-3 in vitro and significant protection against apoptosis in a camptothecin-induced Jurkat T cells system. Among the tested compounds, compound 5i exhibited the most potent caspase-3 inhibitory activity (IC50=1.15 nM). The molecular docking predicted the interactions and binding modes of the synthesized inhibitor in the caspase-3 active site.
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