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  • Carbonic anhydrase activators: activation of human isozymes I, II and IX with phenylsulfonylhydrazido l-histidine derivatives.

Carbonic anhydrase activators: activation of human isozymes I, II and IX with phenylsulfonylhydrazido l-histidine derivatives.

Bioorganic & medicinal chemistry letters (2009-04-07)
Marie-Rose Abdo, Daniela Vullo, Mohamed-Chiheb Saada, Jean-Louis Montero, Andrea Scozzafava, Jean-Yves Winum, Claudiu T Supuran
摘要

Activation of the human carbonic anhydrase (CA, EC 4.2.1.1) isozymes I, II (cytosolic) and IX (transmembrane, tumor-associated isoform) with a series of arylsulfonylhydrazido-l-histidines incorporating 4-substituted-phenyl, pentafluorophenyl- and beta-naphthyl moieties was investigated. The compounds showed a weak hCA I activation profile, but were more efficient as hCA II and IX activators. The 4-iodophenyl-substituted derivative behaved as a strong and isozyme selective hCA II activator, with an activation constant of 0.21muM. This is the first isoform-selective, potent CA activator reported to date.

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