Abstract
The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Enzyme Activation / drug effects
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Inhibitory Concentration 50
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JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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Molecular Structure
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology
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Structure-Activity Relationship
Substances
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Protein Kinase Inhibitors
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Pyrazoles
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Pyrimidines
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pyrazole
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JNK Mitogen-Activated Protein Kinases