Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors. Issue 11 (1st June 2020)

• Record Type: Journal Article
• Authors: Grandane, Aiga; Nocentini, Alessio; Werner, Thomas; Zalubovskis, Raivis; Supuran, Claudiu T.
• Is Part Of: Bioorganic & medicinal chemistry. Volume 28:Issue 11(2020)
• Publication Date: 2020-06-01
• Subjects: Carbonic anhydrase -- Benzoxepinone -- Selective inhibitor -- Tumor -- Catalytic Wittig reaction; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2020.115496
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: Abstract: 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.