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

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

Volume: 8 Issue: 6

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

Affiliation:

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

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.

Cite this article as:

Raza Rabia, Saeed Aamer, Lecka Joanna, Sevigny Jean and Iqbal Jamshed, Identification of Small Molecule Sulfonic Acids as Ecto-5'-Nucleotidase Inhibitors, Medicinal Chemistry 2012; 8(6) . https://dx.doi.org/10.2174/1573406411208061133