Abstract
We have developed a family of 4-benzimidazolyl-N-piperazinethyl-pyrimidin-2-amines that are subnanomolar inhibitors of Lck. A subset of these Lck inhibitors, with heterocyclic substituents at the benzimidazole C5, are also low-nanomolar inhibitors of cellular IL2 release.
MeSH terms
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Inhibitory Concentration 50
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Interleukin-2 / antagonists & inhibitors
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Interleukin-2 / metabolism
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors*
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / metabolism*
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Molecular Structure
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacology*
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Pyrimidines / chemistry*
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Pyrimidines / pharmacology*
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Structure-Activity Relationship
Substances
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Interleukin-2
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Protein Kinase Inhibitors
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Pyrimidines
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck)