Microwave-assisted synthesis and bioevaluation of new sulfonamides
| Autor: | Cem Yamali, Kaan Kucukoglu, Fatma Yesilyurt, Hiroshi Sakagami, İlhami Gülçin, Mustafa Gul, Claudiu T. Supuran, Halise Inci Gul |
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| Rok vydání: | 2017 |
| Předmět: |
microwave
Stereochemistry Cell Survival Pyrazoline Nerve Tissue Proteins 01 natural sciences Medicinal chemistry chemistry.chemical_compound Carbonic anhydrase Cell Line Tumor Drug Discovery sulfonamide polycyclic compounds Humans Carbonic Anhydrase I Enzyme Inhibitors Cytotoxicity Microwaves pyrazoline Pharmacology chemistry.chemical_classification Sulfonamides biology Molecular Structure 010405 organic chemistry Chemistry lcsh:RM1-950 General Medicine Carbon-13 NMR 0104 chemical sciences Sulfonamide Enzyme Activation 010404 medicinal & biomolecular chemistry lcsh:Therapeutics. Pharmacology biology.protein Proton NMR cytotoxicity Biological Assay Selectivity Carrier Proteins Adenylyl Cyclases Research Article |
| Zdroj: | Journal of Enzyme Inhibition and Medicinal Chemistry Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 369-374 (2017) |
| DOI: | 10.6084/m9.figshare.4725685 |
| Popis: | In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) 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 9 (PSE = 4.2), 12 (PSE = 4.1) and 13 (PSE = 3.9) with the highest potency selectivity expression (PSE) values in cytotoxicity experiments and the compounds 13 (Ki = 3.73 ± 0.91 nM toward hCA I) and 14 (Ki = 3.85 ± 0.57 nM toward hCA II) with the lowest Ki values in CA inhibition studies can be considered as leader compounds for further studies. |
| Databáze: | OpenAIRE |
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