Abstract
We have developed a series of 4-thiophenoxy-N-(3,4,5-trialkoxyphenyl) pyrimidine-2-amines as potent and selective inhibitors of p56lck tyrosine kinase activity. In particular, the most potent inhibitor shows cellular activity in T-cell receptor (TCR) stimulated models of cytokine release, which suggests an immunomodulatory role for this class of inhibitor.
Keywords: Trialkoxyphenyl, tyrosine, T-cell, pyrimidine-2-amines
Current Medicinal Chemistry
Title: 4-Thiophenoxy-N-(3,4,5-Trialkoxyphenyl)Pyrimidine-2-Amines as Potent and Selective Inhibitors of the T-Cell Tyrosine Kinase p56lck
Volume: 11 Issue: 6
Author(s): D. F.C. Moffat, R. A. Allen, S. E. Rapecki, P. D. Davis, J. O'Connell, M. C. Hutchings, M. A. King, B. A. Boyce and M. J. Perry
Affiliation:
Keywords: Trialkoxyphenyl, tyrosine, T-cell, pyrimidine-2-amines
Abstract: We have developed a series of 4-thiophenoxy-N-(3,4,5-trialkoxyphenyl) pyrimidine-2-amines as potent and selective inhibitors of p56lck tyrosine kinase activity. In particular, the most potent inhibitor shows cellular activity in T-cell receptor (TCR) stimulated models of cytokine release, which suggests an immunomodulatory role for this class of inhibitor.
Export Options
About this article
Cite this article as:
Moffat F.C. D., Allen A. R., Rapecki E. S., Davis D. P., O'Connell J., Hutchings C. M., King A. M., Boyce A. B. and Perry J. M., 4-Thiophenoxy-N-(3,4,5-Trialkoxyphenyl)Pyrimidine-2-Amines as Potent and Selective Inhibitors of the T-Cell Tyrosine Kinase p56lck, Current Medicinal Chemistry 2004; 11 (6) . https://dx.doi.org/10.2174/0929867043455710
DOI https://dx.doi.org/10.2174/0929867043455710 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
- Announcements
Related Articles
-
Resistin: An Inflammatory Cytokine. Role in Cardiovascular Diseases, Diabetes and the Metabolic Syndrome
Current Pharmaceutical Design Study on Transcriptional Responses and Identification of Ribosomal Protein Genes for Potential Resistance against Brown Planthopper and Gall Midge Pests in Rice
Current Genomics Anti-Inflammatory Mechanisms of Glucocorticoids Targeting Granulocytes
Current Drug Targets - Inflammation & Allergy New Perspectives of Infections in Cardiovascular Disease
Current Cardiology Reviews Potential Use of Dendritic Cells for Anti-Atherosclerotic Therapy
Current Pharmaceutical Design The Vpu Protein: New Concepts in Virus Release and CD4 Down-Modulation
Current HIV Research Molecular Mechanisms of Epithelial Regeneration and Neovascularization During Healing of Gastric and Esophageal Ulcers
Current Medicinal Chemistry Hemopoiesis in Ph-Negative Chronic Myeloproliferative Disorders
Current Stem Cell Research & Therapy miRNA and Proteomic Dysregulation in Non-Small Cell Lung Cancer in Response to Cigarette Smoke
MicroRNA Transition Metals for Conjugation of Polyunsaturated Acids and their Esters
Current Organic Chemistry Clozapine Safety, 35 Years Later
Current Drug Safety Attacking HIV Provirus: Therapeutic Strategies to Disrupt Persistent Infection
Infectious Disorders - Drug Targets Inhaled KMUP-1 Prevents Allergic Pulmonary Vascular Inflammation and Remodeling via NO and Suppressed MMP-9 and ICAM-1/VCAM-1
Inflammation & Allergy - Drug Targets (Discontinued) Functional Properties of Pentacyclic Triterpenes Contained in "Orujo" Olive Oil
Current Nutrition & Food Science Management of Complicated Pneumonia in Childhood: A Review of Recent Literature
Reviews on Recent Clinical Trials Metaxalone Suppresses Production of Inflammatory Cytokines Associated with Painful Conditions in Mouse Macrophages RAW264.7 Cells <i>in Vitro</i>: Synergistic Effect with β-caryophyllene
Current Molecular Medicine MRP4/ABCC4 As a New Therapeutic Target: Meta-Analysis to Determine cAMP Binding Sites as a Tool for Drug Design
Current Medicinal Chemistry Warming Up to New Possibilities with the Capsaicin Receptor TRPV1: mTOR, AMPK, and Erythropoietin
Current Neurovascular Research Cox Inhibitors as Potential Chemotherapic Drugs for Mesothelioma
Current Respiratory Medicine Reviews Population Based Helicobacter pylori Screening and Eradication: Advances Versus Side Effects
Current Pharmaceutical Design