Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones
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Erişim
info:eu-repo/semantics/openAccessTarih
2019Yazar
Bilginer, SinanGul, Halise Inci
Erdal, Feyza Sena
Sakagami, Hiroshi
Levent, Serkan
Gulcin, Ilhami
Supuran, Claudiu T.
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In this study, new chalcone compounds having the chemical structure of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones (1?8) were synthesised and were characterised by H-1-NMR, C-13?-NMR, and HRMS spectra. Cytotoxic and carbonic anhydrase (CA) inhibitory effects of the compounds were investigated. Cytotoxicity results pointed out that compound 4, 6-[3-(4-trifluoromethylphenyl)-2-propenoyl]-3H-benzoxazol-2-one, showed the highest cytotoxicity (CC50) and potency-selectivity expression (PSE) value, and thus can be considered as a lead compound of this study. According to the CA inhibitory results, IC50 values of the compounds 1?8 towards hCA I were in the range of 29.74?69.57??M, while they were in the range of 18.14 ? 48.46??M towards hCA II isoenzyme. K-i values of the compounds 1?8 towards hCA I were in the range of 28.37???6.63?70.58???6.67??M towards hCA I isoenzyme and they were in the range of 10.85???2.14 ? 37.96???2.36??M towards hCA II isoenzyme.