Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.
Bioorg Med Chem Lett
; 18(11): 3224-9, 2008 Jun 01.
Article
in En
| MEDLINE
| ID: mdl-18479916
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrroles
/
Urea
/
Proto-Oncogene Proteins c-met
/
Protein Kinase Inhibitors
/
Aminopyridines
Type of study:
Prognostic_studies
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2008
Document type:
Article
Affiliation country:
Estados Unidos