Yamali, CemGül, Halise İnciÖzli, GülsenAngeli, AndreaKırmızıbayrak, Petek BallarTepedelen, Burcu ErbaykentSakagami, HiroshiBua, SilviaSupuran, Claudiu T.2024-06-252024-06-252021-08-050045-2068https://doi.org/10.1016/j.bioorg.2021.105194https://www.sciencedirect.com/science/article/pii/S004520682100571Xhttps://hdl.handle.net/11452/42368A series of novel N-aryl-1-(4-sulfamoylphenyl)-5-(thiophen-2-yl)-1H-pyrazole-3-carboxamides was synthesized and examined as inhibitors of cytosolic (human) hCA I and hCA II, and cancer-related transmembrane hCA IX and hCA XII isoenzymes. AC2 was the most selective inhibitor towards cancer-related hCA IX while AC8 and AC9 selectively inhibited hCA XII over off-target isoenzymes. Anticancer effects of the compounds were evaluated towards human oral squamous cell carcinoma (OSCC) cell lines, human mesenchymal normal oral cells, breast (MCF7), prostate (PC3), non-small cell lung carcinoma cells (A549), and non-tumoral fetal lung fibroblast cells (MRC5). Compounds moderately showed cytotoxicity towards cancer cell lines. Among others, AC6 showed cell specific cytotoxic activity and induced apoptosis in a dose-dependent manner without a significant change in the cell cycle distribution of MCF7. These results suggest that pyrazole-3-carboxamides need further molecular modification to increase their anticancer drug candidate potency.eninfo:eu-repo/semantics/closedAccessAntiproliferative activityHca ixBioactivitiesChalconesApoptosisCarbonic anhydraseAnticancerPyrazoleBenzenesulfonamideCarboxamideApoptosis, cell cycleScience & technologyLife sciences & biomedicinePhysical sciencesBiochemistry & molecular biologyChemistry, organicChemistryArticle00070551330000411510.1016/j.bioorg.2021.1051941090-2120