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

…, M Koenig, Y He, T Vojkovsky, P LoGrasso…

文献索引：Shin, Youseung; Chen, Weiming; Habel, Jeff; Duckett, Derek; Ling, Yuan Yuan; Koenig, Marcel; He, Yuanjun; Vojkovsky, Tomas; LoGrasso, Philip; Kamenecka, Theodore M. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 12 p. 3344 - 3347

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被引用次数: 19

摘要

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.