期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 32, 期 1, 页码 369-374出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2016.1254207
关键词
Carbonic anhydrase; cytotoxicity; microwave; pyrazoline; sulfonamide
资金
- Research Foundation of Ataturk University, Turkey [2012/74]
In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by H-1 NMR, C-13 NMR and HRMS. Cytotoxic activities and inhibitory effects on carbonic anhydrase I and II isoenzymes of the compounds were investigated. The compounds 9 (PSE = 4.2), 12 (PSE = 4.1) and 13 (PSE = 3.9) with the highest potency selectivity expression (PSE) values in cytotoxicity experiments and the compounds 13 (Ki = 3.73 +/- 0.91 nM toward hCA I) and 14 (Ki = 3.85 +/- 0.57 nM toward hCA II) with the lowest Ki values in CA inhibition studies can be considered as leader compounds for further studies.
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