Home | Articles
Published on:November 2021
Indian Journal of Pharmaceutical Education and Research, 2021; 55(3s):S807-S813
Original Article | doi:10.5530/ijper.55.3s.188

Synthesis, Cytotoxic and Antihyperlipidemic Activities of Some New coumarinyl 4-Thiazolidinone Derivatives


Authors and affiliation (s):

Katte Ishwar Bhat, Abhishek Kumar*, Pankaj Kumar

Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Deralakatte, Mangaluru, Karnataka, INDIA.

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.

Key words: Coumarins, Schiff bases, 4-Thiazolidinones, Cytotoxic activity, Antihyperlipidemic activity.

 




 

Impact Factor

IJPER - An Official Publication of Association of Pharmaceutical Teachers of India is pleased to announce continued growth in the Latest Release of Journal Citation Reports (source: Web of Science Data).

 

Impact Factor® as reported in the 2020 Journal Citation Reports® (Clarivate Analytics, 2021): 0.638

The Official Journal of Association of Pharmaceutical Teachers of India (APTI)
(Registered under Registration of Societies Act XXI of 1860 No. 122 of 1966-1967, Lucknow)

Indian Journal of Pharmaceutical Education and Research (IJPER) [ISSN-0019-5464] is the official journal of Association of Pharmaceutical Teachers of India (APTI) and is being published since 1967.

DOI HISTORY

IJPER uses reference linking service using Digital Object Identifiers (DOI) by Crossref. Articles from the year 2013 are being assigned DOIs for its permanent URLs