Abstract
The synthesis and abl tyrosine kinase inhibitory activities of alkyltriazenes conjugated to phenylaminopyrimidines are described. Significant abl inhibitory activities were observed only when a benzamido spacer was inserted between the 1,2,3-triazene chain and the 2-phenyaminopyridopyrimidine moiety.
MeSH terms
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Drug Delivery Systems / methods*
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Enzyme Inhibitors / administration & dosage
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Enzyme Inhibitors / chemical synthesis
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Fusion Proteins, bcr-abl
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Protein-Tyrosine Kinases / antagonists & inhibitors*
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Protein-Tyrosine Kinases / metabolism
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Pyridines / administration & dosage
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Pyridines / chemical synthesis*
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Pyrimidinones / administration & dosage
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Pyrimidinones / chemical synthesis*
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Triazenes / administration & dosage
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Triazenes / chemical synthesis*
Substances
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Enzyme Inhibitors
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Pyridines
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Pyrimidinones
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Triazenes
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Protein-Tyrosine Kinases
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Fusion Proteins, bcr-abl