Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors

Journal Article · Mon Sep 14 00:00:00 EDT 2009 · Bioorg. Med. Chem. Lett.

DOI:https://doi.org/10.1016/j.bmcl.2009.03.086· OSTI ID:1005841

Shin, Youseung; Chen, Weiming; Habel, Jeff; Duckett, Derek; Ling, Yuan Yuan; Koenig, Marcel; He, Yuanjun; Vojkovsky, Tomas; LoGrasso, Philip; Kamenecka, Theodore M

A novel series of c-jun N-terminal kinase (JNK) inhibitors were designed and developed from a high-throughput-screening hit. Through the optimization of the piperazine amide 1, several potent compounds were discovered. The X-ray crystal structure of 4g showed a unique binding mode different from other well known JNK3 inhibitors.

• Research Organization: Argonne National Laboratory (ANL)
• Sponsoring Organization: USDOE
• OSTI ID: 1005841
• Journal Information: Bioorg. Med. Chem. Lett., Journal Name: Bioorg. Med. Chem. Lett. Journal Issue: (12) ; 06, 2009 Vol. 19; ISSN 0960-894X
• Country of Publication: United States
• Language: ENGLISH

Related Subjects

36 MATERIALS SCIENCE
AMIDES
CRYSTAL STRUCTURE
OPTIMIZATION
PHOSPHOTRANSFERASES
PIPERAZINES
SYNTHESIS