Publication: Indole-Based Hydrazones Containing A Sulfonamide Moiety as Selective Inhibitors of Tumor-Associated Human Carbonic Anhydrase Isoforms IX and XII
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Date
2019-05-01
Authors
Authors
Demir-Yazici, Kubra
BUA, Silvia
Akgunes, Nurgul Mutlu
Akdemir, ATİLLA
Supuran, Claudiu T.
Guzel-Akdemir, Ozlen
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Abstract
Novel sulfonamidoindole-based hydrazones with a 2-(hydrazinocarbonyl)-3-phenyl-1Hindole-5-sulfonamide scaffold were synthesized and tested in enzyme inhibition assays against the
tumor-associated carbonic anhydrase isoforms, hCA IX and XII, and the off-targets, hCA I and II.
The compounds showed selectivity against hCA IX and XII over hCA I and II. Six compounds showed
KI values lower than 10 nM against hCA IX or XII. Molecular modeling studies were performed to
suggest binding interactions between the ligand and the hCA active sites.
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Citation
Demir-Yazici K., BUA S., Akgunes N. M. , Akdemir A., Supuran C. T. , Guzel-Akdemir O., -Indole-Based Hydrazones Containing A Sulfonamide Moiety as Selective Inhibitors of Tumor-Associated Human Carbonic Anhydrase Isoforms IX and XII-, INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, cilt.20, 2019