Synthesis, Cytotoxic and Antihyperlipidemic Activities of Some New coumarinyl 4-Thiazolidinone Derivatives
Katte Ishwar Bhat1, Abhishek Kumar1★, Pankaj Kumar1★ Corresponding author
- 1Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte, Mangaluru, Karnataka, INDIA.
CORRESPONDENCE
Abhishek Kumar
Assistant Professor, Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University) Paneer, Deralakatte, Mangaluru- 575018, Karnataka, INDIA.
Received: 15-01-2021; Revised: 16-02-2021; Accepted: 09-08-2021.
Volume 55, Issue 3S · pp. S807–S813 · PUBLISHED 2021 · DOI: 10.5530/ijper.55.3s.188
ABSTRACT
Background: Despite tremendous advancements both in early diagnosis and approaches to treatment, cancer still remains an unconquered problem. The development of new chemotherapeutic agents for the treatment of cancer with fewer side effects is an important goal for medicinal chemists. Hyperlipidemia is a worth-mentioning risk factor in quickly expanding cardiovascular diseases, including myocardial infarction and, furthermore, in stroke. Hence, there is a need to develop new cytotoxic and antihyperlipidemic drugs. Materials and Methods: In the present study, a series of new substituted 2-(4-hydroxy-2-oxo-2H-chromen-3-yl)-2-methyl-3-phenylthiazolidin-4-one (TKA1-TKA13) were synthesized by reacting various 4-hydroxy-3-(1-(phenylimino) ethyl)-2H-chromen-2-one with thioglycollic acid. The intermediate 4-hydroxy-3-(1-(phenylimino) ethyl)-2H-chromen-2-one (SKA1-SKA13) were synthesized by reacting 4-hydroxyl coumarin with various substituted anilines in alcohol medium. All the newly synthesized compounds were assigned on the basis of IR, 1H NMR and mass spectral data. Results: The newly synthesized compounds were evaluated for in-vitro cytotoxic activity using Methyl Thiazolyl Tetrazolium (MTT) assay and in-vitro antihyperlipidemic activity by HMG-CoA reductase assay. Compound TKA12 possess potent cytotoxic activity on lung adenocarcinoma cells in a concentration dependent manner compared to the standard cisplatin. Most of the compounds showed potent antihyperlipidemic activity comparable with that of the standard pravastatin. Conclusion: The in-vitro results suggest that most of the compounds may be a promising antihyperlipidemic molecules and compound TKA12 showed potent cytotoxic activity which can be further determined by in vivo studies.
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Bhat, K. I., Kumar, A., & Kumar, P. (2021). Synthesis, Cytotoxic and Antihyperlipidemic Activities of Some New coumarinyl 4-Thiazolidinone Derivatives. Indian Journal of Pharmaceutical Education and Research, 55(3S), S807–S813. https://doi.org/10.5530/ijper.55.3s.188