Abstract
A new class of benzimidazolone p38 MAP kinase inhibitors was discovered through high-throughput screening. X-ray crystallographic data of the lead molecule with p38 were used to design analogues with improved binding affinity and potency in a cell assay of LPS-induced TNFalpha production. Herein, we report the SAR of this new class of p38 inhibitors.
MeSH terms
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Benzimidazoles / chemical synthesis
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Benzimidazoles / pharmacology*
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Crystallography, X-Ray
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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Models, Molecular
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Molecular Conformation
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Protein Conformation
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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p38 Mitogen-Activated Protein Kinases / chemistry*
Substances
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Benzimidazoles
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Enzyme Inhibitors
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benzimidazole
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p38 Mitogen-Activated Protein Kinases