期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 20, 期 9, 页码 -出版社
MDPI
DOI: 10.3390/ijms20092354
关键词
carbonic anhydrase; sulfonamides; hydrazones; enzyme inhibition; molecular modeling
资金
- Istanbul University Scientific Research Projects Department [TSA-2019-30535]
Novel sulfonamidoindole-based hydrazones with a 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-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 K-I 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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