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Synthesis, Cytotoxicity and 99Mtc-Mibi Tumor Cell Uptake Evaluation of 2-Phenylbenzothiazole Tagged Triazole Derivatives Publisher Pubmed



M Aghaei Khouzani MARZIEH ; Z Noaparast ZOHREH ; T Asadi TINA ; S Saeidi SAJAD ; A Heidarnia ALIREZA ; B Hamzeh Moghadam BEHNOUSH ; H Mosavi Kia HANIEH ; Sm Hashemi Seyedeh MAHDIEH ; M Mahdavic MOHAMMAD
Authors

Source: Future Medicinal Chemistry Published:2024


Abstract

Aim: The extensive utilization of 2-phenylbenzothiazole due to their wide array of biological activities, particularly in cancer therapy, has caused great attention to explore more potent derivatives. Materials & methods: We report the synthesis of 2-phenylbenzothiazole tagged 1,2,3-triaozle (8) through Cu(I)-catalyzed cycloaddition of alkyne side chain with aryl-substituted azides. Results: The in vitro experiments, using MTT and 99mTc-MIBI cell uptake methods, demonstrated the remarkable anticancer activity of these compounds against A549, SKOV3 and MCF7 cell lines. Conclusion: Compounds 8b, 8f and 8i possessed high cytotoxic activity as compared with doxorubicin. Compound 8g has a similar inhibitory effect on the proliferation of breast cancer cells as doxorubicin. In silico study indicated that compound 8 would be a good lead for the development of new potent anticancer agents. © 2024 Elsevier B.V., All rights reserved.
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