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Publikācija: N-Substituted and Ring Opened Saccharin Derivatives Selectively Inhibit Transmembrane

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Publikācijas valoda English (en)
Nosaukums oriģinālvalodā N-Substituted and Ring Opened Saccharin Derivatives Selectively Inhibit Transmembrane, Tumor-Associated Carbonic Anhydrases IX and XII
Pētniecības nozare 1. Dabaszinātnes
Pētniecības apakšnozare 1.4. Ķīmija
Autori Jekaterīna Ivanova
Fabrizio Carta
Daniela Vullo
Janis Leitans
Andris Kazaks
Kaspars Tārs
Raivis Žalubovskis
Claudiu T. Supuran
Atslēgas vārdi Carbonic anhydrase | Inhibitor | Isoform selectivity | Saccharin | Secondary/tertiary sulfonamide
Anotācija A series of N-substituted saccharins incorporating aryl, alkyl and alkynyl moieties, as well as some ring opened derivatives were prepared and investigated as inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). The widespread cytosolic isoforms CA I and II were not inhibited by these sulfonamides whereas transmembrane, tumor-associated ones were effectively inhibited, with K I s in the range of 22.1–481 nM for CA IX and of 3.9–245 nM for hCA XII. Although the inhibition mechanism of these tertiary/secondary sulfonamides is unknown for the moment, the good efficacy and especially selectivity for the inhibition of the tumor-associated over the cytosolic, widespread isoforms, make these derivatives of considerable interest as enzyme inhibitors with various pharmacologic applications.
DOI: 10.1016/j.bmc.2017.04.007
Hipersaite: http://www.sciencedirect.com/science/article/pii/S0968089617305254?via%3Dihub 
Atsauce Ivanova, J., Carta, F., Vullo, D., Leitans, J., Kazaks, A., Tārs, K., Žalubovskis, R., Supuran, C. N-Substituted and Ring Opened Saccharin Derivatives Selectively Inhibit Transmembrane, Tumor-Associated Carbonic Anhydrases IX and XII. Bioorganic and Medicinal Chemistry, 2017, Vol.25, No.13, 3583.-3589.lpp. ISSN 0968-0896. Pieejams: doi:10.1016/j.bmc.2017.04.007
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ID 26427