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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Identification of Small Molecule Sulfonic Acids as Ecto-5'-Nucleotidase Inhibitors

Author(s): Rabia Raza, Aamer Saeed, Joanna Lecka, Jean Sevigny and Jamshed Iqbal

Volume 8, Issue 6, 2012

Page: [1133 - 1139] Pages: 7

DOI: 10.2174/1573406411208061133

Price: $65


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 Ki value of 0.66 M and 19 (N-(4- sulfamoylphenylcarbamothioyl) pivalamide) with Ki value of 0.78 M 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.

Keywords: Adenosine, Ecto-5'-Nucleotidase, Enzyme inhibition, Enzyme kinetics, Sulfonic acid derivatives, Suramin

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