Microwave-assisted synthesis and bioevaluation of new sulfonamides

Abstract

<p>In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1<i>H</i>-pyrazol-1-yl]benzenesulfonamide derivatives (<b>8-14</b>) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. Cytotoxic activities and inhibitory effects on carbonic anhydrase I and II isoenzymes of the compounds were investigated. The compounds <b>9</b> (PSE = 4.2), <b>12</b> (PSE = 4.1) and <b>13</b> (PSE = 3.9) with the highest potency selectivity expression (PSE) values in cytotoxicity experiments and the compounds <b>13</b> (<i>Ki</i> = 3.73 ± 0.91 nM toward hCA I) and <b>14</b> (<i>Ki</i> = 3.85 ± 0.57 nM toward hCA II) with the lowest <i>Ki</i> values in CA inhibition studies can be considered as leader compounds for further studies.</p