Pala, Nicolino and Micheletto, Laura and Sechi, Mario and Aggarwal, Mayank and Carta, Fabrizio and McKenna, Robert and Supuran, Claudiu T. (2013) Carbonic anhydrase inhibition with benzenesulfonamides and tetrafluorobenzenesulfonamides obtained via click chemistry. ACS Medicinal Chemistry Letters, Vol. 5 (8), p. 927-930. eISSN 1948-5875. Article.
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A series of novel benzene- and 2,3,5,6-tetrafluorobenzenesulfonamide was synthesized by using a click chemistry approach starting from azido-substituted sulfonamides and alkynes, incorporating aryl, alkyl, cycloalkyl, and amino-/hydroxy-/halogenoalkyl moieties. The new compounds were medium potency inhibitors of the cytosolic carbonic anhydrase (CA, EC 22.214.171.124) isoforms I and II and low nanomolar/subnanomolar inhibitors of the tumor-associated hCA IX and XII isoforms. The X-ray crystal structure of two such sulfonamides in adduct with hCA II allowed us to understand the factors governing inhibitory power.
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