7-Aryl-triazolyl-substituted sulfocoumarins are potent,selective inhibitors of the tumor-associated carbonic anhydrase IX and XII |
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| Authors: | Alessio Nocentini Mariangela Ceruso Claudiu T Supuran |
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| Institution: | 1. University of Florence, Neurofarba Department, Sesto Fiorentino, Firenze, Italy and;2. University of Florence, Dipartimento di Chimica “U. Schiff”, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino, Firenze, Italy;3. University of Florence, Neurofarba Department, Sesto Fiorentino, Firenze, Italy and;4. University of Florence, Dipartimento di Chimica “U. Schiff”, Laboratorio di Chimica Bioinorganica, Sesto Fiorentino, Firenze, Italy |
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| Abstract: | 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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| Keywords: | Carbonic anhydrase click chemistry human carbonic anhydrase IX human carbonic anhydrase XII sulfocoumarin tumor-associated isoforms |
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