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

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 c...
Ausführliche Beschreibung

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 (IC50 =1.15nM). The molecular docking predicted the interactions and binding modes of the synthesized inhibitor in the caspase-3 active site. Ausführliche Beschreibung