Key result
Compound 20d, a novel isatin-sulphonamide derivative, exhibited moderate inhibitory activity against caspase-3 with an IC50 of 2.33 µM in vitro.
A new series of isatin-sulphonamide derivatives were synthesized and identified as moderate caspase inhibitors, with compound 20d showing promising activity supported by molecular docking.
Isatin-sulphonamide caspase inhibitors require in vivo validation; leaves open therapeutic translation in apoptosis-driven cardiovascular disease.
ABTRACTIn this paper, a new series of isatin-sulphonamide based derivatives were designed, synthesised and evaluated as caspase inhibitors. The compounds containing 1-(pyrrolidinyl)sulphonyl and 2-(phenoxymethyl)pyrrolidin-1-yl)sulphonyl substitution at C5 position of isatin core exhibited better results compared to unsubstituted derivatives. According to the results of caspase inhibitory activity, compound 20d showed moderate inhibitory activity against caspase-3 and −7 in vitro compared to Ac-DEVD-CHO (IC50 = 0.016 ± 0.002 μM). Among the studied compounds, some active inhibitors with IC50s in the range of 2.33–116.91 μM were identified. The activity of compound 20d was rationalised by the molecular modelling studies exhibiting the additional van der Waals interaction of N-phenylacetamide substitution along with efficacious T-shaped π-π and pi-cation interactions. The introduction of compound 20d with good caspase inhibitory activity will help researchers to find more potent agents.
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Firoozpour et al. (2020) studied this question. Compound 20d (isatin-sulphonamide derivative) vs. Ac-DEVD-CHO was evaluated on Caspase-3 inhibitory activity (IC50 in µM). Compound 20d, a novel isatin-sulphonamide derivative, exhibited moderate inhibitory activity against caspase-3 with an IC50 of 2.33 µM in vitro.
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