Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

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

Sumathy Arunachalam^1,2 , Suresh Ramalingam², Gowrishankar Narayanasamy Lachmanan¹, Srinivasan Nagarajan²

¹Department of Pharmaceutical Chemistry, Prime College of Pharmacy, Palakkad, Kerala, India; ²Department of Pharmacy, Faculty of Engineering and Technology, Annamalai University, Chidambaram, Tamilnadu, India.

For correspondence:- Sumathy Arunachalam Email: sumathy512@gmail.com

Published: 30 November 2022

Citation: Arunachalam S, Ramalingam S, Lachmanan GN, Nagarajan S. Design and characterization of core scaffold pyrazolone fused thiazolidinone analogues as potent anticancer agents. Trop J Pharm Res 2022; 21(11):2429-2437 doi: 10.4314/tjpr.v21i11.23

© 2022 The authors.
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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.

Keywords: Pyrazolone, Thiazolidinone scaffolds, HER2, EFGR inhibitors, GLIDE XP, In vitro cytotoxicity, MCF-7 cell line