New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors |
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| Authors: | M. Alexandra Esteves Osvaldo Ortet Anabela Capelo Claudiu T. Supuran Sérgio M. Marques M. Amélia Santos |
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| Affiliation: | 1. LNEG, Unidade de Pilhas de Combustível e Hidrogénio, Estrada do Paço do Lumiar, 1649-038 Lisboa, Portugal;2. Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy;3. Instituto Superior Técnico, Centro de Química Estrutural, Av. Rovisco Pais 1, 1049-001 Lisboa, Portugal |
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| Abstract: | A set of benzenesulfonamide (BSA) derivatives bearing a hydroxypyrimidinone (HPM) moiety were synthesized and investigated for their inhibitory activity against several carbonic anhydrase (CA, EC 4.2.1.1) isozymes. They all revealed to be very potent inhibitors (nanomolar order) of the cytosolic CA I and II isozymes, but especially of the transmembrane, tumor-associated CA IX isozyme, a beneficial feature for a potential antitumor effect of these compounds. Further structure optimization aimed at improving the specificity of CA inhibition and enhancing their matrix metalloproteinase (MMP) inhibitory activity may also lead to new compounds with an attractive dual mechanism of action as antitumor agents. |
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