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Published on:December 2020
Indian Journal of Pharmaceutical Education and Research, 2020; 54(4):1121-1132
Original Article | doi:10.5530/ijper.54.4.208

Synthesis, in-silico Studies and Evaluation of Anticancer Activity of Some Novel Benzothiazole Substituted 4-Thiazolidinones


Authors and affiliation (s):

Chaithra Raju Shetty1, Katte Ishwar Bhat1,*, Abhishek Kumar1, Pankaj Kumar1, Praveen Thaggikuppe Krishnamurthy2, Vijay Kumar Merugumolu3

1Department of Pharmaceutical Chemistry, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Mangaluru, Karnataka, INDIA.

2Department of Pharmacology, JSS College of Pharmacy, Ooty, The Nilgiris, Tamil Nadu, INDIA.

3Department of Pharmacology, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Paneer, Mangaluru, Karnataka, INDIA.

Abstract:

Background: Cancer is one of the leading diseases associated with the high degree of mortality. In current scenario chemotherapy is the major treatment for cancer and it still has few limitations. The continuous seek for highly effective and safe anticancer agents is the one of the major goal for medicinal chemists. Objectives: In the present work, the hybrid molecule i.e benzothiazole substituted 4-thiazolidinone has been synthesized and evaluated for anticancer activity. Methods: A series of novel benzothiazole substituted 4-thiazolidinone derivatives were synthesized by reacting 2-amino-6-methyl benzothiazole with aromatic aldehydes in alcoholic media, resulting schiff bases are made to react with thioglycolic acid in dioxane. Characterization of synthesized compounds were done by IR, 1H NMR, Mass spectroscopy. In silico studies with molecular docking was performed for the synthesized derivatives by taking proteins from PDB i.e VEGFR-2 kinase and Human thymidylate synthase (PDB ID:2QU5 and 5HS3) as the targets. Results and Discussion: Based on the docking score, best four compounds were selected and screened for in-vitro anticancer activity. From the in-vitro data, finally one potential molecule was selected and evaluated for in-vivo cytotoxic activity. Conclusion: All 4 screened derivatives were found to show good cytotoxic activity, out of which P14 can be considered as promising molecule.

Key words: Benzothiazole, 4-Thiazolidinone, Anticancer, In silico, Docking.

 




 

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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.

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