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

[ Vol. 8 , Issue. 6 ]

Author(s):

Rabia Raza, Aamer Saeed, Joanna Lecka, Jean Sevigny and Jamshed Iqbal   Pages 1133 - 1139 ( 7 )

Abstract:


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

Affiliation:

Department of Pharmaceutical Sciences,COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan.



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