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
Medicinal Chemistry
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.
Export Options
About this article
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
DOI https://dx.doi.org/10.2174/1573406411208061133 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Interpreting the Mechanisms by which Integrins Promote the Differentiation of Mesenchymal Stem Cells and Integrin Application Prospects
Current Stem Cell Research & Therapy Phytoestrogens and Mitochondrial Biogenesis in Breast Cancer. Influence of Estrogen Receptors Ratio
Current Pharmaceutical Design Influence of Polymer Molecular Weight on in-vitro Characteristics and Cytotoxicity of Fulvestrant Loaded Nanoparticles
Current Drug Therapy Biomimetic Drug Delivery Systems Oriented by Biological Function in Tumor Targeting
Current Drug Targets Deciphering the Systems Biology of mTOR Inhibition by Integrative Transcriptome Analysis
Current Pharmaceutical Design Lipoidal-Nano Architecture for Parental Drug Delivery: Formulation Development and Regulatory Concerns
Current Applied Polymer Science BRCA1-Associated Triple-Negative Breast Cancer and Potential Treatment for Ruthenium-Based Compounds
Current Cancer Drug Targets Nucleic Acid Aptamers as Novel Class of Therapeutics to Mitigate Alzheimer’s Disease Pathology
Current Alzheimer Research Non-viral Gene Delivery and Therapeutics Targeting to Brain
Current Nanoscience MicroRNAs as Regulators in Normal Hematopoietic and Leukemia Stem Cells: Current Concepts and Clinical Implications
Current Molecular Medicine Recent Patents and Patent Applications Relating to mTOR Pathway
Recent Patents on DNA & Gene Sequences Preventive and Protective Roles of Dietary Nrf2 Activators Against Central Nervous System Diseases
CNS & Neurological Disorders - Drug Targets Multifunctional Proteins in Tumorigenesis: Aminoacyl-tRNA Synthetases and Translational Components
Current Proteomics Tamoxifen and its New Derivatives in Cancer Research
Recent Patents on Anti-Cancer Drug Discovery Editorial [Hot Topic: Novel Kinase Inhibitors in Cancer Therapy (Guest Editors: Ezra E.W. Cohen and Nikolai G. Rainov)]
Reviews on Recent Clinical Trials The Emerging Role of Stereotactic Radiosurgery in the Treatment of Glioblastoma Multiforme
Current Radiopharmaceuticals Rho GTPase Activating Proteins in Cancer Phenotypes
Current Protein & Peptide Science Activation of Sphingosine Kinase-1 in Cancer: Implications for Therapeutic Targeting
Current Molecular Pharmacology Pharmacological Properties and Therapeutic Potential of Naringenin: A Citrus Flavonoid of Pharmaceutical Promise
Current Pharmaceutical Design Nanotools for the Delivery of Antimicrobial Peptides
Current Drug Targets