4-Thiophenoxy-N-(3,4,5-Trialkoxyphenyl)Pyrimidine-2-Amines as Potent and Selective Inhibitors of the T-Cell Tyrosine Kinase p56lck

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, M. J. Perry.

Journal Name: Current Medicinal Chemistry

Volume 11 , Issue 6 , 2004

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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

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Article Details

VOLUME: 11
ISSUE: 6
Year: 2004
Page: [747 - 753]
Pages: 7
DOI: 10.2174/0929867043455710
Price: $58