Abstract
Facile synthesis of two new series of tetracyclic azepine and oxazocine analogs is described. These analogs were evaluated for their potential as MAPKAP-K2 (MK2) inhibitors and several were found to be potent at inhibiting MK2 with a non-ATP competitive binding mode.
Published by Elsevier Ltd.
MeSH terms
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Azepines / chemical synthesis
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Azepines / chemistry
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Azepines / pharmacology*
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Humans
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Intracellular Signaling Peptides and Proteins / antagonists & inhibitors*
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Molecular Structure
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Oxazocines / chemical synthesis
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Oxazocines / chemistry
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Oxazocines / pharmacology*
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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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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Azepines
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Intracellular Signaling Peptides and Proteins
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Oxazocines
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Protein Kinase Inhibitors
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MAP-kinase-activated kinase 2
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Protein Serine-Threonine Kinases