title: Microwave-assisted synthesis and bioevaluation of new sulfonamides.
abstract: 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 by1H 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.
authors.affiliation: a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ataturk University , Erzurum , Turkey.
authors.forename: Halise Inci
authors.initials: HI
authors.lastname: Gul
authors.affiliation: a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ataturk University , Erzurum , Turkey.
authors.forename: Cem
authors.initials: C
authors.lastname: Yamali
authors.affiliation: a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ataturk University , Erzurum , Turkey.
authors.forename: Fatma
authors.initials: F
authors.lastname: Yesilyurt
authors.affiliation: b Division of Pharmacology , Meikai University School of Dentistry , Sakado , Saitama , Japan.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Sakagami
authors.affiliation: a Department of Pharmaceutical Chemistry, Faculty of Pharmacy , Ataturk University , Erzurum , Turkey.
authors.forename: Kaan
authors.initials: K
authors.lastname: Kucukoglu
authors.affiliation: c Department of Chemistry, Faculty of Science , Ataturk University , Erzurum , Turkey.|d Department of Zoology, College of Science , King Saud University , Riyadh , Saudi Arabia.
authors.forename: Ilhami
authors.initials: I
authors.lastname: Gulcin
authors.affiliation: e Department of Physiology, Faculty of Medicine , Ataturk University , Erzurum , Turkey.
authors.forename: Mustafa
authors.initials: M
authors.lastname: Gul
authors.affiliation: f Neurofarba Departmente Laboratorio di Chimica Bioinorganica , Universita degli Studi di Firenze , Sesto Fiorentino , Florence , Italy.
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism; D001681:Biological Assay; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D006801:Humans; D008872:Microwaves; D015394:Molecular Structure; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000145:classification / Q000494:pharmacology* / Q000633:toxicity; D009687:Nuclear Proteins
chemical_list: D000262:Adenylyl Cyclases; D002352:Carrier Proteins; D004791:Enzyme Inhibitors; D009419:Nerve Tissue Proteins; D013449:Sulfonamides; C484328:MAGEE1 protein, human; D009687:Nuclear Proteins; C579271:ADCY10 protein, human
keywords: Carbonic anhydrase; cytotoxicity; microwave; pyrazoline; sulfonamide