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
-
Anti-diabetic Drug Metformin: Challenges and Perspectives for Cancer Therapy
Current Cancer Drug Targets Genomic Expression in the Epileptogenic Hippocampus and Psychiatric Co-Morbidities
Current Psychiatry Reviews NUPR1 Interacts with p53, Transcriptionally Regulates p21 and Rescues Breast Epithelial Cells from Doxorubicin-Induced Genotoxic Stress
Current Cancer Drug Targets Cancer Drug Discovery Targeting Histone Methyltransferases: An Update
Current Medicinal Chemistry Light Chain LC and TAT-EGFP-HCS of Botulinum Toxin Expression and Biological Function <i>in vitro</i> and <i>in vivo</i>
Current Proteomics Targeting Hypoxia for Sensitization of Tumors to Radio- and Chemotherapy
Current Cancer Drug Targets Evaluation of Dendrimer Safety and Efficacy through Cell Line Studies
Current Drug Targets Molecular Imaging of Brain Tumors Personal Experience and Review of the Literature
Current Molecular Medicine Cholesterol in Alzheimers Disease: Unresolved Questions
Current Alzheimer Research Targeting Tumor Microenvironment with Silibinin: Promise and Potential for a Translational Cancer Chemopreventive Strategy
Current Cancer Drug Targets Recent Advances in Targeted Therapy for Glioma
Current Medicinal Chemistry Natural Sirtuin Modulators in Drug Discovery: A Review (2010 -2020)
Current Medicinal Chemistry Oncogenic MicroRNA-27a is a Target for Genistein in Ovarian Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry microRNA Biogenesis Pathway as a Therapeutic Target for Human Disease and Cancer
Current Pharmaceutical Design Imaging Adoptive Cell Transfer Based Cancer Immunotherapy
Current Pharmaceutical Biotechnology Targeting the Phosphatidylinositol 3-Kinase/Akt/Mammalian Target of Rapamycin Signaling Network in Cancer Stem Cells
Current Medicinal Chemistry Dual Targeting of Glioma U251 Cells with Nanoparticles Prevents Tumor Angiogenesis and Inhibits Tumor Growth
Current Neurovascular Research Involvement of Cysteine Proteases in Cancer
Current Medicinal Chemistry Fusogenic Oncolytic Herpes Simplex Viruses as a Potent and Personalized Cancer Vaccine
Current Pharmaceutical Biotechnology Potential Impacts of Prebiotics and Probiotics on Cancer Prevention
Anti-Cancer Agents in Medicinal Chemistry