In this study, new 4-[3-(aryl)-5-substitutedphenyl-4,5-dihydro-1H-pyrazole-1-yl]benzensulfonamides (19–36) were synthesized and evaluated their cytotoxic/anticancer and CA inhibitory effects. According to results obtained, the compounds 34 (4-[5-(2,3,4-trimethoxyphenyl)-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-yl] benzensulfonamide, Potency-Selectivity Expression (PSE) = 141) and 36 (4-[5-(3,4,5-trimethoxyphenyl)-3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazole-1-yl]benzensulfonamide, PSE = 54.5) were found the leader anticancer compounds with the highest PSE values. In CA inhibitory studies, the compounds 36 and 24 (4-[5-(3,4,5-trimethoxyphenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-yl]benzensulfonamide) were found the leader CA inhibitors depending on selectivity ratios. The compound 36 was a selective inhibitor of hCA XII isoenzyme (hCA I/hCA XII = 1250 and hCA II/hCA XII = 224) while the compound 24 was a selective inhibitor of hCA IX isoenzyme (hCA I/hCA IX = 161 and hCA II/hCA IX = 177). The compounds 24, 34, and 36 can be considered to develop new anticancer drug candidates.

在这项研究中，新的4- [3-（芳基）-5-取代苯基-4,5-二氢-1- ħ -吡唑-1-基] benzensulfonamides（19 - 36）的合成和评价了它们的细胞毒性/抗肿瘤和CA抑制效果。根据获得的结果，化合物34（4- [5-（2,3,4-三甲氧基苯基）-3-（噻吩-2-基）-4,5-二氢-1 H-吡唑-1-基]苯甲磺酰胺，效能选择性表示（PSE）= 141）和36（4- [5-（3,4,5-三甲氧基苯基）-3-（噻吩-2-基）-4,5-二氢-1 H-吡唑-已发现1-yl]苯磺酰胺（PSE = 54.5）是具有最高PSE值的主要抗癌化合物。在CA抑制研究中，化合物36和24（4- [5-（3,4,5-三甲氧基苯基）-3-（4-氟苯基）-4,5-二氢-1 H-吡唑-1-基]苯磺酰胺被发现是领先的CA抑制剂，取决于选择性比率。化合物36是hCA XII同工酶的选择性抑制剂（hCA I / hCA XII = 1250和hCA II / hCA XII = 224），而化合物24是hCA IX同工酶的选择性抑制剂（hCA I / hCA IX = 161和hCA II / hCA IX = 177）。化合物24，34和36可以被认为是开发新的抗癌药物候选。