ArticleJournal of enzyme inhibition and medicinal chemistry2022
Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors.
Article in Journal of enzyme inhibition and medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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8 citing papers in PubMed.
- Unraveling the Potential of Amino‑, Acylamino‑, and Ureido-Substituted 3ACS medicinal chemistry letters · 2025Article
- Isocoumarins incorporating chalcone moieties act as isoform selective tumor-associated carbonic anhydrase inhibitors.Future medicinal chemistry · 2024Article
- 1,3-Diaryl Triazenes Incorporating Disulfonamides Show Both Antiproliferative Activity and Effective Inhibition of Tumor-associated Carbonic Anhydrases IX and XII.Anti-cancer agents in medicinal chemistry · 2024Article
- Aryl derivatives of 3Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Derivatives of 4-methyl-1,2,3-benzoxathiazine 2,2-dioxide as selective inhibitors of human carbonic anhydrases IX and XII over the cytosolic isoforms I and II.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Potent carbonic anhydrase I, II, IX and XII inhibition activity of novel primary benzenesulfonamides incorporating bis-ureido moieties.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Tail-Approach-Based Design and Synthesis of Coumarin-Monoterpenes as Carbonic Anhydrase Inhibitors and Anticancer Agents.ACS omega · 2023Article
- Inhibition studies of the protozoan α-carbonic anhydrase fromJournal of enzyme inhibition and medicinal chemistry · 2022Article
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5 authors.
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Abstract
Isocoumarins, isomeric to comarins which act as effective carbonic anhydrase (CA, EC 4.2.1.1) inhibitors, were investigated for the first time as inhibitors of this enzyme. A series of 3-substituted and 3,4-disubstituted isocoumarins incorporating phenylhydrazone, 1-phenyl-pyrazole and pyrazolo-substituted pyrimidine trione/thioxo-pyrimidine dione moieties were investigated for their interaction with four human (h) CA isoforms, hCA I, II, IX and XII, known to be important drug targets. hCA I and II were not inhibited by these compounds, whereas hCA IX and XII were inhibited in the low micromolar range by the less bulky derivatives. The inhibition constants ranged between 2.7-78.9 µM against hCA IX and of 1.2-66.5 µM against hCA XII. As for the coumarins, we hypothesise that the isocoumarins are hydrolysed by the esterase activity of the enzyme with formation of 2-carboxy-phenylacetic aldehydes which act as CA inhibitors. Isocoumarins represent a new class of CA inhibitors.
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