Abstract
Synthesis of hybrids of 1-deoxynojirimycin (DNJ) and 5-aryl-1,2,3-triazole as potential bifunctional inhibitors of angiogenesis is described. The DNJ component inhibits the biosynthesis of cell surface oligosaccharides necessary for angiogenesis, whereas the aryl-1,2,3-triazole inhibits methionine aminopeptidase II, a target in angiogenesis therapy. One bifunctional compound was a more potent inhibitor of angiogenesis in vitro than DNJ alone or the 5-aryl-1,2,3-triazole alone.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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1-Deoxynojirimycin / chemical synthesis*
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1-Deoxynojirimycin / chemistry
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1-Deoxynojirimycin / pharmacology*
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Aminopeptidases / antagonists & inhibitors*
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Angiogenesis Inhibitors / chemical synthesis*
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Angiogenesis Inhibitors / chemistry
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Angiogenesis Inhibitors / pharmacology*
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Animals
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Endothelial Cells / drug effects
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Glycoside Hydrolase Inhibitors*
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Humans
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Metalloendopeptidases / antagonists & inhibitors*
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Mice
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Models, Molecular*
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Molecular Structure
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacology*
Substances
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Angiogenesis Inhibitors
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Glycoside Hydrolase Inhibitors
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Triazoles
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1-Deoxynojirimycin
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Aminopeptidases
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methionine aminopeptidase 2
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Metalloendopeptidases