Abstract
In an effort to understand the effect of N-alkylation of triarylimidazoles on Tie2 inhibition, ortho-substituted C-2 aryl analogs were synthesized to investigate the effect of different torsion angles on potency. This exercise resulted in the identification of a potent and selective tetrasubstituted imidazole that was efficacious in an animal model of angiogenesis.
MeSH terms
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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Inhibitory Concentration 50
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Methylation
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Models, Molecular
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Molecular 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 / pharmacology*
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Receptor, TIE-2 / antagonists & inhibitors*
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Receptor, TIE-2 / chemistry
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Receptor, TIE-2 / metabolism
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Sensitivity and Specificity
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Structure-Activity Relationship
Substances
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Imidazoles
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Protein Kinase Inhibitors
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imidazole
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Receptor, TIE-2