Design and characterization of core scaffold pyrazolone fused thiazolidinone analogues as potent anticancer agents

Abstract

Purpose: To synthesize novel pyrazolone fused thiazolidinone analogues and evaluate their efficiency as potent HER2 and EGFR inhibitors in human breast adenocarcinoma cells for anti-cancer activity. Method: In this study, several pyrazolone fused thiazolidinone analogues were synthesized, and characterized by elemental analysis, IR, 1H-NMR, 13C-NMR, and mass spectroscopy, as well as tested for their in vitro cytotoxicity against breast cancer cell line (MCF-7) by MTT assay. A correlation study of the cytotoxicity was performed to obtain the Docking score using Schrodinger (Maestro) Version 9.6 Glide XP software. Result: A total of 10 compounds were synthesised and analysed for their physiochemical, spectral, and cytotoxic activity against breast cancer cell lines (MCF-7). Among the synthesised compounds, compound 4B5 showed significantly higher (p < 0.05) anticancer properties against MCF-7 cell lines with docking score of -6.614, and half-maximal concentration (IC50) value of 001.17 M compared to other synthesized compounds of the same categories. Conclusion: Novel pyrazolone-fused thiazolidinone analogues have been successfully synthesized. The synthesised compounds possess anti-cancer activity against the MCF-7 cell lines. This could potentially lead to the development of new anti-breast cancer agents.