Abstract
The synthesis and characterization of a novel polycyclic azaindole based derivative is disclosed, and its binding to JAK2 is described. The compound is further evaluated for its ability to block the EPO/JAK2 signaling cascade in vitro and in vivo.
MeSH terms
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Animals
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Aza Compounds / chemical synthesis
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Aza Compounds / chemistry*
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Aza Compounds / pharmacokinetics
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Aza Compounds / pharmacology*
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Cell Line, Tumor
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Crystallography, X-Ray
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Erythropoietin / metabolism
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacokinetics
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Indoles / pharmacology*
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Janus Kinase 2 / antagonists & inhibitors*
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Janus Kinase 2 / metabolism
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Lactams, Macrocyclic / chemical synthesis
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Lactams, Macrocyclic / chemistry
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Lactams, Macrocyclic / pharmacokinetics
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Lactams, Macrocyclic / pharmacology
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Male
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Mice
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Mice, Inbred BALB C
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Mice, SCID
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Models, Molecular
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Molecular Conformation
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Protein Conformation
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacokinetics
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Protein Kinase Inhibitors / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Signal Transduction / drug effects
Substances
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Aza Compounds
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Indoles
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Lactams, Macrocyclic
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Protein Kinase Inhibitors
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Erythropoietin
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Janus Kinase 2