論文 - 詳細
| RRC ID | 59950 |
|---|---|
| 著者 | Bilginer S, Gul HI, Erdal FS, Sakagami H, Levent S, Gulcin I, Supuran CT. |
| タイトル | Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones. |
| ジャーナル | J Enzyme Inhib Med Chem |
| Abstract |
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 1H-NMR, 13 C-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 µM, while they were in the range of 18.14 - 48.46 µM towards hCA II isoenzyme. Ki
values of the compounds 1-8 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. |
| 巻・号 | 34(1) |
| ページ | 1722-1729 |
| 公開日 | 2019-12-1 |
| DOI | 10.1080/14756366.2019.1670657 |
| PMID | 31576761 |
| PMC | PMC6781194 |
| MeSH | Antineoplastic Agents / chemical synthesis* Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacology* Antineoplastic Agents / toxicity Benzoxazoles / chemical synthesis* Benzoxazoles / chemistry Benzoxazoles / pharmacology* Benzoxazoles / toxicity Carbonic Anhydrase Inhibitors / chemical synthesis* Carbonic Anhydrase Inhibitors / chemistry Carbonic Anhydrase Inhibitors / pharmacology* Carbonic Anhydrase Inhibitors / toxicity Carbonic Anhydrases / metabolism Cell Line, Tumor Cell Survival / drug effects Chalcone / chemistry Child Drug Screening Assays, Antitumor / methods Female Humans Isoenzymes / metabolism Molecular Structure Structure-Activity Relationship |
| IF | 4.673 |
| 引用数 | 3 |
| リソース情報 | |
| ヒト・動物細胞 | HSC-2(RCB1945) |