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oai:ebyu-rdlopen.rawdatalibrary.net:ebyu/130502026-10-18T21:13:26Zopenairedrivercom_ebyu_10000col_ebyu_10001

Exploring of tumor-associated carbonic anhydrase isoenzyme IX and XII inhibitory effects and cytotoxicities of the novel N-aryl-1-(4-sulfamoylphenyl)-5-(thiophen-2-yl)-1H-pyrazole-3-carboxamidesYamali, CemInci Gul, HaliseOzli, GulsenAngeli, AndreaBallar Kirmizibayrak, PetekErbaykent Tepedelen, BurcuSakagami, HiroshiBua, SilviaSupuran, Claudiu T.AnticancerApoptosis, cell cycleBenzenesulfonamideCarbonic anhydraseCarboxamidePyrazoleAntigens, NeoplasmAntineoplastic AgentsApoptosisCarbonic Anhydrase InhibitorsCarbonic Anhydrase IXCarbonic AnhydrasesCell Line, TumorHumansNeoplasmsPyrazolesacetazolamideantineoplastic agentcarbonate dehydratase IXcarbonate dehydratase XIIdoxorubicinfluorouracilmelphalann aryl 1 (4 sulfamoylphenyl) 5 (thiophen 2 yl) 1h pyrazole 3 carboxamideunclassified drugCA9 protein, humancarbonate dehydratasecarbonate dehydratase inhibitorpyrazole derivativetumor antigenA 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. © 2021 Elsevier Inc.Academic Press Inc.2021Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/13050https://doi.org/10.1016/j.bioorg.2021.1051940045-2068enBioorganic Chemistryinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/13050