Benzoxepinones: A new isoform-selective class of tumor associated carbonic anhydrase inhibitors
Aiga Grandane1, Alessio Nocentini2, Thomas Werner3
1Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia.
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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