Abstract
The MAP kinase p38 has been implicated in cytokine signaling, and its inhibitors are potentially useful for the treatment of arthritis and osteoporosis. Novel small-molecule inhibitors of p38 kinase were derived from a combinatorial chemistry effort and exhibit activity in the nanomolar range. Very steep structure-activity relationships are observed within this class.
MeSH terms
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Antirheumatic Agents / chemical synthesis
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Antirheumatic Agents / chemistry
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Combinatorial Chemistry Techniques
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Heterocyclic Compounds / chemistry
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Humans
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Hydrocarbons, Chlorinated / chemistry
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Inhibitory Concentration 50
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Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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Osteoporosis / drug therapy
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Phenylurea Compounds / chemical synthesis
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Phenylurea Compounds / pharmacology
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases
Substances
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Antirheumatic Agents
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Enzyme Inhibitors
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Heterocyclic Compounds
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Hydrocarbons, Chlorinated
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Phenylurea Compounds
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Mitogen-Activated Protein Kinases
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p38 Mitogen-Activated Protein Kinases