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• W3081248824 endingPage "104204" @default.
• W3081248824 startingPage "104204" @default.
• W3081248824 abstract "Building on the conclusions of previous inhibition studies with pyridinium-benzenesulfonamides from our team and on the X-ray crystal structure of the lead compound identified, a series of 24 pyridinium derivatives of 3-aminobenzenesulfonamide was synthesized and investigated for carbonic anhydrase inhibition. The new pyridinium-sulfonamides were evaluated as inhibitors of four human carbonic anhydrase (CA, EC 4.2.1.1) isoforms, namely CA I, CA II (cytosolic), CA IX and XII (transmembrane, tumor-associated forms). Excellent inhibitory activity in the nanomolar range was observed against CA IX with most of these sulfonamides, and against CA XII (nanomolar/sub-nanomolar) with some of the new compounds. These sulfonamides were generally potent inhibitors of CA II and CA I too. Docking studies revealed a preference of these compounds to bind the P1 hydrophobic site of CAs, supporting the observed inhibition profile. The salt-like nature of these positively charged sulfonamides can further focus the inhibitory ability on membrane-bound CA IX and CA XII and could efficiently decrease the viability of three human carcinomas under hypoxic conditions where these isozymes are over-expressed, thus recommending the new compounds as potential diagnostic tools or therapeutic agents." @default.
• W3081248824 created "2020-09-01" @default.
• W3081248824 creator A5006759876 @default.
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• W3081248824 date "2020-10-01" @default.
• W3081248824 modified "2023-09-25" @default.
• W3081248824 title "Pyridinium derivatives of 3-aminobenzenesulfonamide are nanomolar-potent inhibitors of tumor-expressed carbonic anhydrase isozymes CA IX and CA XII" @default.
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• W3081248824 doi "https://doi.org/10.1016/j.bioorg.2020.104204" @default.
• W3081248824 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/7846937" @default.
• W3081248824 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32891000" @default.
• W3081248824 hasPublicationYear "2020" @default.
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