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Synonyms: 4-fluorophenylureido-benzenesulfonamide | compound 7 [PMID: 21361354] | SLC0111
Compound class: Synthetic organic
Comment: SLC-0111 is a carbonic anhydrase (CA) IX/XII inhibitor that is being investigated for anti-neoplastic potential [1,4]. SLC-0111 is selective for the transmembrane CA isoforms IX and XII, compared to the cytosolic CA I and II isoforms. CA IX and XII are expressed predominantly in the hypoxic tumour microenvironment. Their inhibition promotes a significant antitumour/antimetastatic effect and reduces cancer stem cell numbers. The crystal structure of SLC-0111 bound to CA II has been resolved (see PDB ID 3N4B) .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Carta F, Vullo D, Osman SM, AlOthman Z, Supuran CT. (2017)
Synthesis and carbonic anhydrase inhibition of a series of SLC-0111 analogs.
Bioorg. Med. Chem., 25 (9): 2569-2576. [PMID:28347633]
2. Congiu C, Onnis V, Deplano A, Balboni G, Dedeoglu N, Supuran CT. (2015)
Synthesis of sulfonamides incorporating piperazinyl-ureido moieties and their carbonic anhydrase I, II, IX and XII inhibitory activity.
Bioorg. Med. Chem. Lett., 25 (18): 3850-3. [PMID:26233435]
3. Pacchiano F, Aggarwal M, Avvaru BS, Robbins AH, Scozzafava A, McKenna R, Supuran CT. (2010)
Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted-ureido-benzenesulfonamides and correlate to inhibitor potency.
Chem. Commun. (Camb.), 46 (44): 8371-3. [PMID:20922253]
4. Pacchiano F, Carta F, McDonald PC, Lou Y, Vullo D, Scozzafava A, Dedhar S, Supuran CT. (2011)
Ureido-substituted benzenesulfonamides potently inhibit carbonic anhydrase IX and show antimetastatic activity in a model of breast cancer metastasis.
J. Med. Chem., 54 (6): 1896-902. [PMID:21361354]