Benzoxepinones: A New Isoform-Selective Class of Tumor Associated Carbonic Anhydrase Inhibitors

Bioorganic and Medicinal Chemistry 2020
Aiga Grandane, Alessio Nocentini, Thomas Werner, Raivis Žalubovskis, Claudiu T. Supuran

Benzoxepinones (“homocoumarins”) are identified as a new class of selective inhibitors for tumor associated human carbonic anhydrases (hCA, EC 4.2.1.1) isoforms IX and XII. Similar to coumarins, they do not inhibit or poorly inhibit cytosolic human (h) isoforms hCA I and II, but act as nanomolar inhibitors of the trans-membrane, tumor associated isoforms hCA IX and XII.

Keywords
Benzoxepinone, Carbonic anhydrase, Catalytic Wittig reaction, Selective inhibitor, Tumor
DOI
10.1016/j.bmc.2020.115496
Hyperlink
https://www-sciencedirect-com.resursi.rtu.lv/science/article/pii/S0968089620303175?via%3Dihub

Grandane, A., Nocentini, A., Werner, T., Žalubovskis, R., Supuran, C. Benzoxepinones: A New Isoform-Selective Class of Tumor Associated Carbonic Anhydrase Inhibitors. Bioorganic and Medicinal Chemistry, 2020, Vol. 28, No. 11, Article number 115496. ISSN 0968-0896. e-ISSN 1464-3391. Available from: doi:10.1016/j.bmc.2020.115496

Publication language
English (en)