Abstract
Selective small molecule inhibitors of Tie-2 kinase are important tools for the validation of Tie-2 signaling in pathological angiogenesis. Reported herein is the optimization of a nonselective scaffold into a potent and highly selective inhibitor of Tie-2 kinase.
MeSH terms
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Administration, Oral
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Benzimidazoles / administration & dosage
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology*
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Biological Availability
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Crystallography, X-Ray
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HeLa Cells
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Humans
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Models, Molecular
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Protein Kinase Inhibitors / administration & dosage
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Receptor, TIE-2 / antagonists & inhibitors*
Substances
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Benzimidazoles
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Protein Kinase Inhibitors
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Receptor, TIE-2