Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 32, Issue 1, Pages 169-175Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2016.1243536
Keywords
Benzenesulfonamide; carbonic anhydrase; cytotoxicity; phenol; pyrazoline
Funding
- Ataturk University
- Ministry of Education, Culture, Sports, Science and Technology [Sakagami H. 25670897]
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In this study, 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl] benzenesulfonamide (1-9) types compounds were synthesized and their chemical structures were confirmed by H-1 NMR, C-13 NMR and HRMS spectra. Cytotoxic and carbonic anhydrase (CA) inhibitory effects of the compounds were investigated. Cytotoxicity experiments pointed out that compound 4, (4-[5-(4-chlorophenyl)-3-(4-hydroxyphenyl)-4,5dihydro- pyrazol-1-yl] benzenesulfonamide), exerting the highest tumor selectivity (TS) and potency selectivity expression (PSE) values, can be considered as a lead compound of this study in terms of development of novel anticancer agents. All synthesized sulfonamides showed a good inhibition profile on hCA IX and XII in the range of 53.5-923nM and 6.2-95 nM, respectively. These compounds were 2.5-13.4 times more selective for the inhibition of hCA XII versus hCA IX, except compound 2 which had similar inhibitory action towards both isoenzymes.
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