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 and M. J. Perry   Pages 747 - 753 ( 7 )

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

Affiliation:

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

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