Fluoroenesulphonamides: N -sulphonylurea isosteres showing nanomolar selective cancer-related transmembrane human carbonic anhydrase inhibition - Regenerative Medicine and Skeleton Accéder directement au contenu
Article Dans Une Revue Journal of Enzyme Inhibition and Medicinal Chemistry Année : 2018

Fluoroenesulphonamides: N -sulphonylurea isosteres showing nanomolar selective cancer-related transmembrane human carbonic anhydrase inhibition

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.
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hal-02169774 , version 1 (08-04-2024)

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Benoit Metayer, Andrea Angeli, Agnès Mingot, Kévin Jouvin, Gwilherm Evano, et al.. Fluoroenesulphonamides: N -sulphonylurea isosteres showing nanomolar selective cancer-related transmembrane human carbonic anhydrase inhibition. Journal of Enzyme Inhibition and Medicinal Chemistry, 2018, 33 (1), pp.804-808. ⟨10.1080/14756366.2018.1461097⟩. ⟨hal-02169774⟩
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