Synthesis and Investigation of Cytotoxicity in Different Cell Lines of Novel Hydroxypyranones

Pelin Nur ÜÇKAN, Gülşah Karakaya, Beyza DÜZLEYEN,Canan SEVİMLİ GÜR,Mutlu Dilsiz Aytemir

Hacettepe University Journal of the Faculty of Pharmacy(2023)

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摘要
Mannich bases synthesized from kojic acid have been determined in extensive studies conducted by our study group that they have a wide variety of biological activities. In this study, new anticancer-active compounds were synthesized from compounds with high anticancer activity. The compounds' structures were identified through the utilization of spectroscopic methods and elemental analyses. The cytotoxicity screening of the compounds were done by MTT assay on different human cancer cell lines. Compound 1 bearing iodomethyl moiety, showed remarkable cytotoxicity with IC50 values in the range of 8.11 and 21.24 µg/mL. The IC50 value on Vero (African green monkey kidney epithelial) is over 100 µg/mL which means low cytotoxicity against healthy cells. Compared to this, SK-MEL cells have 12 times less IC50 value, with a therapeutic index over 12. The closest cytotoxic effectivity to KOJI MG84 which is previously reported as a cytotoxic agent, is observed on the SK-MEL cell line in compound 1, with 4 times less cytotoxic activity.
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cytotoxicity
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