期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 31, 期 6, 页码 1226-1233出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2015.1115401
关键词
Carbonic anhydrase; click chemistry; human carbonic anhydrase IX; human carbonic anhydrase XII; sulfocoumarin; tumor-associated isoforms
资金
- Marie Curie ITN FP7 project (Dynano)
Sulfocoumarins behave as interesting inhibitors of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1). Here, we report a new series of 7-substituted derivatives which were obtained by the click chemistry approach from 7-propargyloxy-sulfocoumarin and aryl azides incorporating halogens, hydroxy, methoxy and carboxyl moieties in their molecules. The new compounds were screened for the inhibition on four physiologically relevant human CA (hCA) isoforms, the cytosolic hCA I and II and the transmembrane tumor-associated hCA IX and XII. The new compounds did not inhibit the cytosolic isoforms but were low nanomolar inhibitors of the tumor-associated ones hCA IX and XII.
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