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
-
Dynamic Role of Microparticles in Type 2 Diabetes Mellitus
Current Diabetes Reviews Targeting Therapeutic and Imaging Agents to Folate Receptor Positive Tumors
Current Pharmaceutical Biotechnology Allergic and Photoallergic Contact Dermatitis from Ketoprofen: Evaluation of Cross-Reactivities by a Combination of Photopatch Testing and Computerized Conformational Analysis
Current Pharmaceutical Design Arachidonate Cascade in the Intensive Insulin Therapy for Critically Ill Patients with Sepsis: Roles of Prostaglandins on Hyperglycemia-Impaired Immunity
Letters in Drug Design & Discovery The Potential for Targeting Oncogenic WNT/β -Catenin Signaling in Therapy
Current Drug Targets Genetic Vaccination for the Immunotherapy of B-Cell Malignancies
Current Gene Therapy QSAR and Docking Studies on Propenone Derivatives as Dual COX and 5- LOX Inhibitors
Letters in Organic Chemistry Modifications of the Immune Responsiveness in Patients with Autoimmune Thyroiditis: Evidence for a Systemic Immune Alteration
Current Pharmaceutical Design Cytokines in Colitis-Associated Cancer: Potential Drug Targets?
Inflammation & Allergy - Drug Targets (Discontinued) Effect of Inhibitors of Nitric Oxide in Animal Models and Future Directions for Therapy in Inflammatory Disorders
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents A Walk in Nature: Sesquiterpene Lactones as Multi-Target Agents Involved in Inflammatory Pathways
Current Medicinal Chemistry The Antioxidant Activity of Coumarins and Flavonoids
Mini-Reviews in Medicinal Chemistry Nanocrystals of Glycyrrhetinic Acid: Comparative Efficiency of Particle Size Reduction Techniques
Drug Delivery Letters Endocannabinoid Signaling in Midbrain Dopamine Neurons: More than Physiology?
Current Neuropharmacology Can We Select Patients for Colorectal Cancer Prevention with Aspirin?
Current Pharmaceutical Design Poly (ADP-Ribose) Polymerase-1 (PARP-1) as Immune Regulator
Endocrine, Metabolic & Immune Disorders - Drug Targets Pharmacological Modulation of the State of Awareness in Patients with Disorders of Consciousness: An Overview
Current Pharmaceutical Design GPER and ER: Estrogen Receptors with Distinct Biological Roles in Breast Cancer
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Antioxidants Suppress Th1-Type Immune Response In Vitro
Drug Metabolism Letters Effects of Diet-Derived Molecules on the Tumor Microenvironment
Current Angiogenesis (Discontinued)