Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors

Mahbub Alam; Rebekah E Beevers; Tom Ceska; Richard J Davenport; Karen M Dickson; Mara Fortunato; Lewis Gowers; Alan F Haughan; Lynwen A James; Mark W Jones; Natasha Kinsella; Christopher Lowe; Johannes W G Meissner; Anne-Lise Nicolas; Benjamin G Perry; David J Phillips; William R Pitt; Adam Platt; Andrew J Ratcliffe; Andrew Sharpe; Laura J Tait

doi:10.1016/j.bmcl.2007.03.078

Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3463-7. doi: 10.1016/j.bmcl.2007.03.078. Epub 2007 Mar 30.

Affiliation

¹ UCB, Granta Park, Great Abington, Cambridge CB21 6GS, UK.

PMID: 17459703
DOI: 10.1016/j.bmcl.2007.03.078

Abstract

The development of a series of novel aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, JNK2 and CDK2, and the in vitro inhibitory value for a c-Jun cellular assay are discussed.

MeSH terms

Cyclin-Dependent Kinase 2 / antagonists & inhibitors
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology*
JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors*
Mitogen-Activated Protein Kinase 8 / antagonists & inhibitors
Mitogen-Activated Protein Kinase 9 / antagonists & inhibitors
Models, Chemical
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Mitogen-Activated Protein Kinase 9
Cyclin-Dependent Kinase 2
JNK Mitogen-Activated Protein Kinases
Mitogen-Activated Protein Kinase 8