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

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, H-1-NMR, C-13-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.

Automated summary

Novel pyrazolone fused thiazolidinone analogues were successfully synthesized and evaluated for their inhibition of human breast adenocarcinoma cells. Compound 4B5 showed the highest anticancer properties and has the potential to be developed as a new anti-breast cancer agent.