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Ecto-5'-Nucleotidase inhibitors have great potential as anti-tumor agents. We have investigated biochemical properties of human and rat ecto-5'-Nucleotidases and characterized 19 small molecule sulfonic acid derivatives as potential inhibitors of ecto-5'-Nucleotidases. We identified 11 potent inhibitors of human and rat ecto-5'-Nucleotidases and checked their selectivity. Compound 10 (Sodium 2,4-dinitrobenzenesulfonate) with K(i) value of 0.66 μM and 19 (N-(4-sulfamoylphenylcarbamothioyl) pivalamide) with K(i) value of 0.78 μM were identified as the most potent inhibitors for human and rat ecto-5'-Nucleotidase, respectively. The present compounds have low molecular weights, water solubility and equal potency as compared to the reported inhibitors.


Rabia Raza, Aamer Saeed, Joanna Lecka, Jean Sévigny, Jamshed Iqbal. Identification of small molecule sulfonic acids as ecto-5'-Nucleotidase inhibitors. Medicinal chemistry (Shāriqah (United Arab Emirates)). 2012 Nov;8(6):1133-9

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PMID: 22741787

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