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Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase
- Source :
- Journal of Medicinal Chemistry. 51:2879-2882
- Publication Year :
- 2008
- Publisher :
- American Chemical Society (ACS), 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 :
- Models, Molecular
C-Met
In Vitro Techniques
Crystallography, X-Ray
medicine.disease_cause
Mice
Structure-Activity Relationship
chemistry.chemical_compound
Growth factor receptor
Drug Discovery
medicine
Animals
Phosphorylation
Molecular Structure
Oncogene
Hepatocyte Growth Factor
Chemistry
Kinase
Proto-Oncogene Proteins c-met
Triazoles
Rats
Pyridazines
Biochemistry
Microsomes, Liver
Cancer research
Molecular Medicine
Hepatocyte growth factor
Signal transduction
Carcinogenesis
medicine.drug
Subjects
Details
- ISSN :
- 15204804 and 00222623
- Volume :
- 51
- Database :
- OpenAIRE
- Journal :
- Journal of Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....a031daf87fd230380ea41665042176aa