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Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors
Authors:Youseung Shin  Weiming Chen  Jeff Habel  Derek Duckett  Yuan Yuan Ling  Marcel Koenig  Yuanjun He  Tomas Vojkovsky  Philip LoGrasso  Theodore M Kamenecka
Institution:Department of Molecular Therapeutics, and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way #A2A, Jupiter, FL 33458, United States
Abstract: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.
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