Abstract
A series of indeno[1,2-c]pyrazoles were discovered to be the first known inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase. The synthesis, structure-activity relationship profile, and in-vitro pharmacological characterization of this inaugural series of HRI kinase inhibitors are detailed.
MeSH terms
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Drug Discovery*
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Heme / metabolism*
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Indenes / chemical synthesis
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Indenes / chemistry
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Indenes / pharmacology*
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Models, Molecular
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Molecular Structure
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Molecular Weight
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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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Stereoisomerism
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Structure-Activity Relationship
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eIF-2 Kinase / antagonists & inhibitors*
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eIF-2 Kinase / metabolism
Substances
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Indenes
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Protein Kinase Inhibitors
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Pyrazoles
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Heme
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eIF-2 Kinase