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SYNTHESIS, CYTOTOXIC AND ANTIOXIDANT ACTIVITY OF NEW 1,3-DIMETHYL-8-(CHROMON-3-YL)-XANTHINE DERIVATIVES CONTAINING 2,6-DI-TERT-BUTYLPHENOL FRAGMENTстатья
- Авторы: Shatokhin Stanislav S., Tuskaev Vladislav A., Gagieva Svetlana Ch, Markova Alina A., Pozdnyakov Dmitry I., Denisov Gleb L., Melnikova Elizaveta K., Bulychev Boris M., Oganesyan Eduard T.
- Журнал: New Journal of Chemistry
- Номер: 10
- Год издания: 2021
- Издательство: Royal Society of Chemistry
- Местоположение издательства: United Kingdom
- DOI: 10.1039/D1NJ03726A
- Аннотация: The condensation of 3-formylchromones and 6-amino-5-((3,5-di-tert-butyl-4-oxocyclohexa-2,5-dien-1-ylidene)amino)-1,3-dimethyl-pyrimidine-2,4(1H,3H)-dione allowed us to synthesize chromone based hybrids containing additional pharmacophores - xanthine and sterically hindered phenol fragments. Novel compounds have been characterized by 1H and 13C NMR spectroscopy, mass spectrometry and elemental analysis. The molecular structure of compound 2 was determined by single crystal X-ray diffraction studies. Compounds 2-9, 11, 12exhibit cytotoxic activity against human colon carcinoma cells HCT116 and breast carcinoma cells MCF7 at submicromolar concentrations. Compound 11 containing 6,8-dimethylchromone core has the highest cytotoxicity against tumor cells and lowest at non-tumor fibroblasts - this is leader compound of the obtained series with acceptable in vitro selectivity. Synthesized compounds exhibit antioxidant activity comparable to the reference drug Trolox. Combination of promising antioxidant activity and a selective antitumor cytotoxicity in vitro determines the prospects of these compounds as chemotherapy agents
- Добавил в систему: Гагиева Светлана Черменовна
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| 1. | Risunok_87_1.jpg | Risunok_87_1.jpg | 502,0 КБ | 30 ноября 2021 [GagievaSvetlana1] |