Microwave-assisted synthesis and bioevaluation of new sulfonamides

被引：22

作者：

Gul, Halise Inci ^{[1
]}

Yamali, Cem ^{[1
]}

Yesilyurt, Fatma ^{[1
]}

Sakagami, Hiroshi ^{[2
]}

Kucukoglu, Kaan ^{[1
]}

Gulcin, Ilhami ^{[3
,4
]}

Gul, Mustafa ^{[5
]}

Supuran, Claudiu T. ^{[6
]}

机构：

[1] Ataturk Univ, Dept Pharmaceut Chem, Fac Pharm, Erzurum, Turkey

[2] Meikai Univ Sch Dent, Div Pharmacol, Sakado, Saitama, Japan

[3] Ataturk Univ, Dept Chem, Fac Sci, Erzurum, Turkey

[4] King Saud Univ, Coll Sci, Dept Zool, Riyadh, Saudi Arabia

[5] Ataturk Univ, Dept Physiol, Fac Med, Erzurum, Turkey

[6] Univ Firenze, Neurofarba Dept, Lab Chim Bioinorgan, Florence, Italy

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2017年 / 32卷 / 01期

关键词：

Carbonic anhydrase; cytotoxicity; microwave; pyrazoline; sulfonamide; CARBONIC-ANHYDRASE INHIBITION; MANNICH-BASES; BIOLOGICAL EVALUATION; DERIVATIVES; CHALCONES; PYRAZOLINES; BIOACTIVITY; APOPTOSIS; IX;

D O I：

10.1080/14756366.2016.1254207

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 H-1 NMR, C-13 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.

引用

页码：369 / 374

页数：6

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