期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 8, 页码 2416-2426出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2014.03.002
关键词
1,2-Benzisothiazol-3-one; Caspase-3; Inhibitors; Apoptosis
资金
- National Biomedical Special Project of International Innovation Park [10ZCKFSY08600]
- National Natural Science Foundation of China [21302139]
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. (C) 2014 Elsevier Ltd. All rights reserved.
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