129841-15-2Relevant academic research and scientific papers
Indole-based hydrazones containing a sulfonamide moiety as selective inhibitors of tumor-associated human carbonic anhydrase isoforms ix and xii
Demir-Yazici, Kübra,Bua, Silvia,Akgünes, Nurgül Mutlu,Akdemir, Atilla,Supuran, Claudiu T.,Güzel-Akdemir, ?zlen
, (2019)
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.
Carbonic anhydrase inhibitors. Interaction of 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide with 12 mammalian isoforms: Kinetic and X-ray crystallographic studies
Guezel, Oezlen,Temperini, Claudia,Innocenti, Alessio,Scozzafava, Andrea,Salman, Aydin,Supuran, Claudiu T.
, p. 152 - 158 (2008/09/18)
2-(Hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide was tested for its interaction with 12 carbonic anhydrase (CA, EC 4.2.1.1) isoforms in the search of compounds with good inhibitory activity against isozymes with medicinal chemistry applications, suc
