Microwave-assisted synthesis and bioevaluation of new sulfonamides
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 carboni...
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| Main Authors: | , , , , , , , |
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| Format: | Book |
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Taylor & Francis Group,
2017-01-01T00:00:00Z.
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|---|---|---|---|
| 001 | doaj_ec4e6f3fdcf0484898c121459b163f1b | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Halise Inci Gul |e author |
| 700 | 1 | 0 | |a Cem Yamali |e author |
| 700 | 1 | 0 | |a Fatma Yesilyurt |e author |
| 700 | 1 | 0 | |a Hiroshi Sakagami |e author |
| 700 | 1 | 0 | |a Kaan Kucukoglu |e author |
| 700 | 1 | 0 | |a Ilhami Gulcin |e author |
| 700 | 1 | 0 | |a Mustafa Gul |e author |
| 700 | 1 | 0 | |a Claudiu T. Supuran |e author |
| 245 | 0 | 0 | |a Microwave-assisted synthesis and bioevaluation of new sulfonamides |
| 260 | |b Taylor & Francis Group, |c 2017-01-01T00:00:00Z. | ||
| 500 | |a 1475-6366 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 10.1080/14756366.2016.1254207 | ||
| 520 | |a 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. | ||
| 546 | |a EN | ||
| 690 | |a Carbonic anhydrase | ||
| 690 | |a cytotoxicity | ||
| 690 | |a microwave | ||
| 690 | |a pyrazoline | ||
| 690 | |a sulfonamide | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 369-374 (2017) | |
| 787 | 0 | |n http://dx.doi.org/10.1080/14756366.2016.1254207 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/ec4e6f3fdcf0484898c121459b163f1b |z Connect to this object online. |