Abstract
Tertiary substituted (fluorinated) benzenesulfonamides were synthesized in superacid HF/SbF5 and tested as inhibitors of human carbonic anhydrases (hCAs, EC 4.2.1.1). Strong selectivity toward tumor-associated hCA IX, without inhibiting the offtarget hCA II, was observed, pointing out to a new mechanism of action compared to classical sulfonamides.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antigens, Neoplasm / chemistry*
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Antigens, Neoplasm / metabolism
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Carbonic Anhydrase II / antagonists & inhibitors
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Carbonic Anhydrase II / metabolism
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Carbonic Anhydrase IX
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Carbonic Anhydrase Inhibitors / chemical synthesis*
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Carbonic Anhydrase Inhibitors / chemistry
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Carbonic Anhydrase Inhibitors / metabolism
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Carbonic Anhydrases / chemistry*
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Carbonic Anhydrases / metabolism
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Humans
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Protein Binding
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry*
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Sulfonamides / metabolism
Substances
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Antigens, Neoplasm
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Carbonic Anhydrase Inhibitors
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Sulfonamides
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Carbonic Anhydrase II
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CA9 protein, human
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Carbonic Anhydrase IX
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Carbonic Anhydrases