1, 2-Benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors

…, Z Yan, X Tang, B Sun, W Liu, H Zhou, C Yang

文献索引：Wu, Lixin; Lu, Meiqi; Yan, Zhihui; Tang, Xiaobin; Sun, Bo; Liu, Wei; Zhou, Honggang; Yang, Cheng Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 8 p. 2416 - 2426

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被引用次数: 6

摘要

Abstract 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 (IC 50= ...