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Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 18:3224-3229
- Publication Year :
- 2008
- Publisher :
- Elsevier BV, 2008.
-
Abstract
- A series of acylurea analogs derived from pyrrolopyridine and aminopyridine scaffolds were identified as potent inhibitors of Met kinase activity. The SAR at various positions of the two kinase scaffolds was investigated. These studies led to the discovery of compounds 3b and 20b, which demonstrated favorable pharmacokinetic properties in mice and significant antitumor activity in a human gastric carcinoma xenograft model.
- Subjects :
- Clinical Biochemistry
Aminopyridines
Pharmaceutical Science
Pharmacology
Biochemistry
Receptor tyrosine kinase
Mice
Structure-Activity Relationship
Stomach Neoplasms
In vivo
Drug Discovery
Animals
Humans
Urea
Pyrroles
Kinase activity
Protein Kinase Inhibitors
Molecular Biology
chemistry.chemical_classification
biology
Kinase
Chemistry
Organic Chemistry
Proto-Oncogene Proteins c-met
Xenograft Model Antitumor Assays
In vitro
Enzyme
Enzyme inhibitor
biology.protein
Molecular Medicine
Signal transduction
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 18
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....a5541a60335288c14cacaac51532ac11