1-Aryl-3,4-dihydroisoquinoline inhibitors of JNK3.
Bioorg Med Chem Lett
; 19(8): 2230-4, 2009 Apr 15.
Article
in En
| MEDLINE
| ID: mdl-19303774
ABSTRACT
A series of 1-aryl-3,4-dihydroisoquinoline inhibitors of JNK3 are described. Compounds 20 and 24 are the most potent inhibitors (pIC50 7.3 and 6.9, respectively in a radiometric filter binding assay), with 10- and 1000-fold selectivity over JNK2 and JNK1, respectively, and selectivity within the wider mitogen-activated protein kinase (MAPK) family against p38alpha and ERK2. X-ray crystallography of 16 reveals a highly unusual binding mode where an H-bond acceptor interaction with the hinge region is made by a chloro substituent.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Mitogen-Activated Protein Kinase 10
/
Protein Kinase Inhibitors
/
Isoquinolines
Limits:
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2009
Document type:
Article
Affiliation country:
United kingdom