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
-
The Guanylyl Cyclase Inhibition by MB as Vasoplegic Circulatory Shock Therapeutical Target
Current Drug Targets Protein Kinases as Tumor Biomarkers and Therapeutic Targets
Current Pharmaceutical Design Targeting STAT1 in Both Cancer and Insulin Resistance Diseases
Current Protein & Peptide Science Role of Amylin and its Receptors in Neurodegeneration
Current Protein & Peptide Science Combined Treatment with PPAR-γ Agonists in Pancreatic Cancer: A Glimmer of Hope for Cancer Therapy?
Current Cancer Drug Targets Managing Clopidogrel Hypersensitivity without Interrupting Therapy: The Toronto Approach
Current Vascular Pharmacology Biomarkers to Assess the Targeting of DNA Repair Pathways to Augment Tumor Response to Therapy
Current Molecular Medicine Enhancing Scoring Performance of Docking-Based Virtual Screening Through Machine Learning
Current Bioinformatics Toxic Shock Syndrome and Persistent Immune Activation in an HIVPositive Patient
Current HIV Research Study the Effect of PG E1 and PGF2α on Male Rat Reproductive Functions
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) New Issues About Melatonin and its Effects on the Digestive System
Current Pharmaceutical Design Noscapine and its Analogs as Chemotherapeutic Agent: Current updates
Current Topics in Medicinal Chemistry Exploring the use of Estrogen & Progesterone Replacement Therapy in Subarachnoid Hemorrhage
Current Drug Safety The Usefulness of the Multiple Allergen Simultaneous Test-Chemiluminescent as Compared to the Phadia Immunocap IgE Test Panel System in Children and Adolescents
Recent Patents on Inflammation & Allergy Drug Discovery COVID-19: An Opinion of Prevention and Dietary Based Management Hypothesis
Coronaviruses Breast Cancer in the Personal Genomics Era
Current Genomics The Possible Involvement of Glycogen Synthase Kinase-3 (GSK-3) in Diabetes, Cancer and Central Nervous System Diseases
Current Pharmaceutical Design Isoflavones and Bone Health
Current Women`s Health Reviews Editorial (Thematic Issue: Novel Inflammatory Biomarkers in Cardiovascular Disease: From Molecular Mechanisms to Therapeutic Targets (Part-II))
Current Medicinal Chemistry ACAT1 as a Therapeutic Target and its Genetic Relationship with Alzheimer's Disease
Current Alzheimer Research