Abstract
This communication details the synthesis, biological activity, and binding mode of a novel class of 2-benzimidazole substituted pyrimidines. The most potent analogs disclosed showed low nanomolar activity for the inhibition of Lck kinase and a representative analog was co-crystallized with Hck (a structurally related member of the Src family kinases).
MeSH terms
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Benzimidazoles / chemistry*
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Hydrogen Bonding
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Inhibitory Concentration 50
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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) / chemical synthesis
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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 / chemical synthesis*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Proto-Oncogene Proteins c-hck / chemistry
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Proto-Oncogene Proteins c-hck / metabolism
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Pyrimidines / chemistry*
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Structure-Activity Relationship
Substances
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Benzimidazoles
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Interleukin-2
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Protein Kinase Inhibitors
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Pyrimidines
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benzimidazole
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck)
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Proto-Oncogene Proteins c-hck
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pyrimidine