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- W2108602087 endingPage "591" @default.
- W2108602087 startingPage "586" @default.
- W2108602087 abstract "Carbonic anhydrases (CAs) are widespread metalloenzymes in higher vertebrates including humans. A series of phenolic compounds, including guaiacol, 4-methylguaiacol, 4-propylguaiacol, eugenol, isoeugenol, vanillin, syringaldehyde, catechol, 3-methyl catechol, 4-methyl catechol and 3-methoxy catechol were investigated for their inhibition of all the catalytically active mammalian isozymes of the Zn2+-containing CA (EC 4.2.1.1). All the phenolic compounds effectively inhibited human carbonic anhydrase isoenzymes (hCA I, II, IX and XII), with Kis in the range of 2.20–515.98 μM. The various isozymes showed diverse inhibition profiles. Among the tested phenolic derivatives, compounds 4-methyl catechol and 3-methoxy catechol showed potent activity as inhibitors of the tumour-associated transmembrane isoforms (hCA IX and XII) in the submicromolar range, with high selectivity. The results obtained from this research may lead to the design of more effective carbonic anhydrase isoenzyme inhibitors (CAIs) based on such phenolic compound scaffolds." @default.
- W2108602087 created "2016-06-24" @default.
- W2108602087 creator A5012797490 @default.
- W2108602087 creator A5035013697 @default.
- W2108602087 creator A5050370140 @default.
- W2108602087 creator A5057610594 @default.
- W2108602087 date "2014-11-06" @default.
- W2108602087 modified "2023-10-12" @default.
- W2108602087 title "Carbonic anhydrase inhibitors: guaiacol and catechol derivatives effectively inhibit certain human carbonic anhydrase isoenzymes (hCA I, II, IX and XII)" @default.
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- W2108602087 doi "https://doi.org/10.3109/14756366.2014.956310" @default.