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Fluoroenesulfonamides: N-Sulfonylurea Isosteres Showing Nanomolar Selective Cancer-Related Transmembrane Human Carbonic Anhydrase Inhibition

par Metayer, Benoit;Angeli, Andrea;Martin-Mingot, Agnès;Jouvin, Kevin;Evano, Gwilherm ;Supuran, Claudiu;Thibaudeau, Sébastien
Référence Journal of enzyme inhibition and medicinal chemistry, 33, page (840-808)
Publication Publié, 2018

Article révisé par les pairs

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Résumé :

After hydrofluorination of ynesulphonamides in superacid or in the presence of hydrofluoric acid/base reagents, a series of α-fluoroenamides has been synthesised and tested for the inhibition of carbonic anhydrase (CA, EC 4.2.1.1) isoforms. This study reveals a new, highly selective family of cancer-related transmembrane human (h) CA IX/XII inhibitors. These original fluorinated ureido isosters do not inhibit the widespread cytosolic isoforms hCA I and II and selectively inhibit the transmembrane cancer-related hCA IX and XII, offering interesting new leads for future studies.