Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
J Med Chem
; 50(6): 1280-7, 2007 Mar 22.
Article
in En
| MEDLINE
| ID: mdl-17300186
ABSTRACT
The Ras/Raf/MEK/ERK signal transduction is a key oncogenic pathway implicated in a variety of human cancers. We have identified a novel series of pyrazolylpyrroles as inhibitors of ERK. Aided by the discovery of two distinct binding modes for the pyrazolylpyrrole scaffold, structure-guided optimization culminated in the discovery of 6p, a potent and selective inhibitor of ERK.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrazoles
/
Pyrroles
/
Mitogen-Activated Protein Kinase 1
/
Quantitative Structure-Activity Relationship
/
Mitogen-Activated Protein Kinase 3
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2007
Document type:
Article
Affiliation country:
United States