Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.
J Med Chem
; 58(4): 1976-91, 2015 Feb 26.
Article
in En
| MEDLINE
| ID: mdl-25603482
Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of (S)-14k, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles, (S)-14k was selected for further preclinical evaluation.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyridones
/
Mitogen-Activated Protein Kinase 1
/
Mitogen-Activated Protein Kinase 3
/
Protein Kinase Inhibitors
/
Small Molecule Libraries
/
Antineoplastic Agents
Limits:
Animals
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2015
Document type:
Article
Affiliation country:
United States
Country of publication:
United States