Abstract
A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.
MeSH terms
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Administration, Oral
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Animals
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Benzimidazoles / administration & dosage
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Benzimidazoles / chemical synthesis*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology*
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Biological Availability
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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Drug Design*
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Female
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Humans
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Mice
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Models, Molecular
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Molecular Structure
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Protein Kinase Inhibitors / administration & dosage
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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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Protein Structure, Tertiary
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Stereoisomerism
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Structure-Activity Relationship
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Xenograft Model Antitumor Assays
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raf Kinases / antagonists & inhibitors*
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raf Kinases / metabolism
Substances
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Benzimidazoles
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Protein Kinase Inhibitors
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raf Kinases