Two series of new 5-benzylidenethiazolidine-2,4-diones bearing benzenesulfonamide moiety were designed and synthesized. The synthesized compounds were evaluated for several biological activities, including cytotoxicity, histone deacetylation, and protein phosphatase 1B (PTP1B) inhibitory effects. It was found that those 5-benzylidenethiazolidine-2,4-diones with a chlorine substituent on the benzenesulfonamide moiety exhibited significant cytotoxicity, comparable to that of SAHA, which was used as a positive control. Several cytotoxic compounds also exhibited inhibitory effects against histone deacetylation, suggesting that these compounds might possess histone deacetylase inhibitory property. On the activity of PTP1B, however, these compounds displayed insignificant inhibitory effects.
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We acknowledge the principal financial supports from the National Foundation for Science and Technology of Vietnam (NAFOSTED, Grant number 104.01-2014.11). The biological study was supported by the Medical Research Center program (MRC, Grant number 2010-0029480).
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Thuan, N.T., Dung, D.T.M., Que, D.N. et al. Synthesis and bioevaluation of new 5-benzylidenethiazolidine-2,4-diones bearing benzenesulfonamide moiety. Med Chem Res 24, 3803–3812 (2015). https://doi.org/10.1007/s00044-015-1422-9