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Comparative Study
, 19 (8), 2230-4

1-Aryl-3,4-dihydroisoquinoline Inhibitors of JNK3

Comparative Study

1-Aryl-3,4-dihydroisoquinoline Inhibitors of JNK3

John A Christopher et al. Bioorg Med Chem Lett.


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.

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