Abstract
A series of 4-azaindole inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and series optimisation was performed on the basis of this structure. Future directions for series development are discussed.
MeSH terms
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Cell Line, Tumor
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Computer Simulation
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Crystallography, X-Ray
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Drug Discovery
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Humans
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacology
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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-met / antagonists & inhibitors*
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Proto-Oncogene Proteins c-met / metabolism
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Structure-Activity Relationship
Substances
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4-azaindole
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Indoles
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Protein Kinase Inhibitors
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Proto-Oncogene Proteins c-met