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.
Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors / Grandane A.; Nocentini A.; Werner T.; Zalubovskis R.; Supuran C.T.. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - ELETTRONICO. - 28:(2020), pp. 115496--. [10.1016/j.bmc.2020.115496]
Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors
Nocentini A.;Supuran C. T.
2020
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.
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