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.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Amides / chemical synthesis*
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Amides / pharmacology
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Crystallography, X-Ray
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Drug Evaluation, Preclinical
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Humans
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JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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Piperazines / chemical synthesis*
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Piperazines / pharmacology
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Protein Binding
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / pharmacology
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Structure-Activity Relationship
Substances
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Amides
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Piperazines
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Protein Kinase Inhibitors
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JNK Mitogen-Activated Protein Kinases