Development of Oxathiino[6,5-b]pyridine 2,2-Dioxide Derivatives as Selective Inhibitors of Tumor-Related Carbonic Anhydrases IX and XII

European Journal of Medicinal Chemistry 2020
Aiga Grandane, Alessio Nocentini, Ilona Domračeva, Raivis Žalubovskis, Claudiu T. Supuran

Oxathiino[6,5-b]pyridine 2,2-dioxides are identified as a new class of isoform-selective nanomolar inhibitors of tumor associated human carbonic anhydrases (hCA) IX and XII. At the same time they do not inhibit or poorly inhibit cytosolic isoforms hCA I and II. Oxathiino[6,5-b]pyridine 2,2-dioxides exhibited good antiproliferative properties on tumor cell lines MCF-7 (Human breast adenocarcinoma), A549 (human lung (alveolar) adenocarcinoma) and HeLa (epithelioid cervix carcinoma).

Keywords
Carbonic anhydrase, Inhibitor, oxathiino[6,5-b]pyridine 2,2-dioxide, Tumor
DOI
10.1016/j.ejmech.2020.112300
Hyperlink
https://www.sciencedirect.com/science/article/pii/S0223523420302695?via%3Dihub

Grandane, A., Nocentini, A., Domračeva, I., Žalubovskis, R., Supuran, C. Development of Oxathiino[6,5-b]pyridine 2,2-Dioxide Derivatives as Selective Inhibitors of Tumor-Related Carbonic Anhydrases IX and XII. European Journal of Medicinal Chemistry, 2020, Vol. 200, Article number 112300. ISSN 0223-5234. e-ISSN 1768-3254. Available from: doi:10.1016/j.ejmech.2020.112300

Publication language
English (en)