%0 Journal Article
%T Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones
%A Claudiu T. Supuran
%A Feyza Sena Erdal
%A Halise Inci Gul
%A Hiroshi Sakagami
%A Ilhami Gulcin
%A Serkan Levent
%A Sinan Bilginer
%J Journal of Enzyme Inhibition and Medicinal Chemistry
%D 2019
%R https://doi.org/10.1080/14756366.2019.1670657
%X Abstract In this study, new chalcone compounds having the chemical structure of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones (1每8) were synthesised and were characterised by 1H-NMR, 13ˋC-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每8 towards hCA I were in the range of 29.74每69.57ˋ米M, while they were in the range of 18.14 每 48.46ˋ米M towards hCA II isoenzyme. Ki values of the compounds 1每8 towards hCA I were in the range of 28.37ˋ㊣ˋ6.63每70.58ˋ㊣ˋ6.67ˋ米M towards hCA I isoenzyme and they were in the range of 10.85ˋ㊣ˋ2.14 每 37.96ˋ㊣ˋ2.36ˋ米M towards hCA II isoenzyme
%U https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1670657