Abstract
Tumorigenesis is a multistep process in which oncogenes play a key role in tumor formation, growth, and maintenance. MET was discovered as an oncogene that is activated by its ligand, hepatocyte growth factor. Deregulated signaling in the c-Met pathway has been observed in multiple tumor types. Herein we report the discovery of potent and selective triazolopyridazine small molecules that inhibit c-Met activity.
MeSH terms
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Animals
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Crystallography, X-Ray
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Hepatocyte Growth Factor / physiology
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In Vitro Techniques
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Mice
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Microsomes, Liver / metabolism
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Models, Molecular
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Molecular Structure
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Phosphorylation
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Proto-Oncogene Proteins c-met / antagonists & inhibitors*
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Proto-Oncogene Proteins c-met / chemistry
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Proto-Oncogene Proteins c-met / metabolism
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Pyridazines / chemical synthesis*
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Pyridazines / chemistry
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Pyridazines / pharmacokinetics
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Pyridazines / pharmacology
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Rats
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Structure-Activity Relationship
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacokinetics
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Triazoles / pharmacology
Substances
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Pyridazines
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Triazoles
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Hepatocyte Growth Factor
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Proto-Oncogene Proteins c-met