Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University , Erzurum , Turkey.
School of Dentistry, Meikai University Research Institute of Odontology (M-RIO), Meikai University , Sakado , Japan.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):1722-1729. doi: 10.1080/14756366.2019.1670657.
In this study, new chalcone compounds having the chemical structure of 6-(3-aryl-2-propenoyl)-2()-benzoxazolones () were synthesised and were characterised by H-NMR, C-NMR, and HRMS spectra. Cytotoxic and carbonic anhydrase (CA) inhibitory effects of the compounds were investigated. Cytotoxicity results pointed out that compound , 6-[3-(4-trifluoromethylphenyl)-2-propenoyl]-3-benzoxazol-2-one, showed the highest cytotoxicity (CC) and potency-selectivity expression (PSE) value, and thus can be considered as a lead compound of this study. According to the CA inhibitory results, IC values of the compounds towards hCA I were in the range of 29.74-69.57 µM, while they were in the range of 18.14 - 48.46 µM towards hCA II isoenzyme. K values of the compounds towards hCA I were in the range of 28.37 ± 6.63-70.58 ± 6.67 µM towards hCA I isoenzyme and they were in the range of 10.85 ± 2.14 - 37.96 ± 2.36 µM towards hCA II isoenzyme.
在这项研究中，合成了具有 6-(3-芳基-2-丙烯酰基)-2()-苯并恶唑酮（）化学结构的新查尔酮化合物，并通过 H-NMR、C-NMR 和 HRMS 光谱进行了表征。研究了化合物的细胞毒性和碳酸酐酶（CA）抑制作用。细胞毒性结果表明，化合物 6-[3-(4-三氟甲基苯基）-2-丙烯酰基]-3-苯并恶唑-2-酮（）表现出最高的细胞毒性（CC）和效力选择性表达（PSE）值，因此可以被认为是本研究的先导化合物。根据 CA 抑制结果，化合物对 hCA I 的 IC 值范围为 29.74-69.57 μM，而对 hCA II 同工酶的 IC 值范围为 18.14-48.46 μM。化合物对 hCA I 的 K 值范围为 28.37±6.63-70.58±6.67 μM 对 hCA I 同工酶，对 hCA II 同工酶的 K 值范围为 10.85±2.14-37.96±2.36 μM。
Zotero 插件