New anticancer drug candidates sulfonamides as selective hCA IX or hCA XII inhibitors
Copyright policy )New anticancer drug candidates sulfonamides as selective hCA IX or hCA XII inhibitors
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.
- Ağrı İbrahim Çeçen University Turkey
- Meikai University Japan
- Atatürk University Turkey
- University of Florence Italy
- New York University Italy
Antineoplastic Agents, Sulfonamide, Pyrazoline, Carbonic anhydrases, Cell Line, Structure-Activity Relationship, Antigens, Neoplasm, Humans, Carbonic Anhydrase IX, Carbonic Anhydrase Inhibitors, Carbonic Anhydrases, Cell Proliferation, Sulfonamides, Dose-Response Relationship, Drug, Molecular Structure, 540, Anticancer; Carbonic anhydrases; Dental cells; Pyrazoline; Sulfonamide, Isoenzymes, Anticancer, Dental cells, Pyrazoles, Drug Screening Assays, Antitumor
Antineoplastic Agents, Sulfonamide, Pyrazoline, Carbonic anhydrases, Cell Line, Structure-Activity Relationship, Antigens, Neoplasm, Humans, Carbonic Anhydrase IX, Carbonic Anhydrase Inhibitors, Carbonic Anhydrases, Cell Proliferation, Sulfonamides, Dose-Response Relationship, Drug, Molecular Structure, 540, Anticancer; Carbonic anhydrases; Dental cells; Pyrazoline; Sulfonamide, Isoenzymes, Anticancer, Dental cells, Pyrazoles, Drug Screening Assays, Antitumor
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