1601403-35-3Relevant academic research and scientific papers
1,2-Benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors
Wu, Lixin,Lu, Meiqi,Yan, Zhihui,Tang, Xiaobin,Sun, Bo,Liu, Wei,Zhou, Honggang,Yang, Cheng
, p. 2416 - 2426 (2014/05/06)
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.
