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

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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: T-cell; Trialkoxyphenyl; pyrimidine-2-amines; tyrosine

Document Type: Review Article


Affiliations: Department of Chemistry, Celltech R & D, 216 Bath Road, Slough, SL1 4EN, UK.

Publication date: March 1, 2004

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