Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3

Britt-Marie Swahn; Yafeng Xue; Erwan Arzel; Elisabet Kallin; Angelika Magnus; Niklas Plobeck; Jenny Viklund

doi:10.1016/j.bmcl.2005.11.039

Design and synthesis of 2'-anilino-4,4'-bipyridines as selective inhibitors of c-Jun N-terminal kinase-3

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1397-401. doi: 10.1016/j.bmcl.2005.11.039. Epub 2005 Dec 5.

Authors

Britt-Marie Swahn¹, Yafeng Xue, Erwan Arzel, Elisabet Kallin, Angelika Magnus, Niklas Plobeck, Jenny Viklund

Affiliation

¹ Department of Medicinal Chemistry, AstraZeneca R&D Södertälje, S-151 85, Södertälje, Sweden. britt-marie.swahn@astrazeneca.com

PMID: 16337120
DOI: 10.1016/j.bmcl.2005.11.039

Abstract

The design and synthesis of a new series of c-Jun N-terminal kinase-3 (JNK3) inhibitors with selectivity against JNK1 are reported. The novel series of substituted 2'-anilino-4,4'-bipyridines were designed based on a combination of hits from high throughput screening and X-ray crystal structure information of compounds crystallized into the JNK3 ATP binding active site.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Aniline Compounds / chemistry*
Animals
Crystallography, X-Ray
Drug Design*
Inhibitory Concentration 50
Mitogen-Activated Protein Kinase 10 / antagonists & inhibitors*
Mitogen-Activated Protein Kinase 10 / chemistry
Mitogen-Activated Protein Kinase 10 / metabolism
Models, Molecular
Protein Structure, Tertiary
Pyridines / chemical synthesis*
Pyridines / chemistry
Pyridines / pharmacology*
Rats
Structure-Activity Relationship

Substances

Aniline Compounds
Pyridines
Mitogen-Activated Protein Kinase 10
aniline