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.
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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 |
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