Abstract
A series of pyrrolo[2,3-d]pyrimidines was synthesized and evaluated as inhibitors of Lck. Lck accommodates a diverse set of substituents at N-7. Altering the substituent at N-7 provided compound 13, an orally available lck inhibitor which inhibited TCR mediated IL-2 production after oral dosing.
MeSH terms
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Humans
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Jurkat Cells
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / analysis*
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology*
Substances
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Enzyme Inhibitors
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Pyrimidines
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck)