Abstract
Conformation restriction of linear N-alkylanilide MK2 inhibitors to their E-conformer was developed. This strategy enabled rapid advance in identifying a series of potent non-ATP competitive inhibitors that exhibited cell based activity in anti-TNFα assay.
Copyright © 2013 Elsevier Ltd. All rights reserved.
MeSH terms
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Adenosine Triphosphate / chemistry
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Adenosine Triphosphate / metabolism
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Anilides / chemical synthesis
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Anilides / chemistry*
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Anilides / metabolism
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Binding, Competitive
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Drug Evaluation, Preclinical
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Humans
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Intracellular Signaling Peptides and Proteins / antagonists & inhibitors*
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Intracellular Signaling Peptides and Proteins / metabolism
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Lactams / chemical synthesis
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Lactams / chemistry*
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Lactams / metabolism
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Protein Binding
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / metabolism
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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Protein Serine-Threonine Kinases / metabolism
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anilides
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Intracellular Signaling Peptides and Proteins
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Lactams
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Protein Kinase Inhibitors
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Adenosine Triphosphate
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MAP-kinase-activated kinase 2
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Protein Serine-Threonine Kinases