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Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2008 May 22; Vol. 51 (10), pp. 2879-82. Date of Electronic Publication: 2008 Apr 22. - Publication Year :
- 2008
-
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.
- Subjects :
- Animals
Crystallography, X-Ray
Hepatocyte Growth Factor physiology
In Vitro Techniques
Mice
Microsomes, Liver metabolism
Models, Molecular
Molecular Structure
Phosphorylation
Proto-Oncogene Proteins c-met chemistry
Proto-Oncogene Proteins c-met metabolism
Pyridazines chemistry
Pyridazines pharmacokinetics
Pyridazines pharmacology
Rats
Structure-Activity Relationship
Triazoles chemistry
Triazoles pharmacokinetics
Triazoles pharmacology
Proto-Oncogene Proteins c-met antagonists & inhibitors
Pyridazines chemical synthesis
Triazoles chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 51
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 18426196
- Full Text :
- https://doi.org/10.1021/jm800043g