Abstract
Several 7-alkoxy-4-anilino-3-quinolinecarbonitriles were synthesized and evaluated for Src kinase inhibitory activity. Optimal inhibition of both Src enzymatic and cellular activity was seen with analogues having a 2,4-dichloro-5-methoxyaniline group at C-4. Compound 18, which has a 1-methylpiperidinemethoxy group at C-7, showed in vivo activity in a xenograft model.
MeSH terms
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Animals
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Cell Line
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Cell Transplantation
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Fibroblasts / enzymology
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Mice
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Mice, Nude
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Nitriles / chemical synthesis*
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Nitriles / pharmacology*
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Quinolines / chemical synthesis*
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Quinolines / pharmacology*
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Rats
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Structure-Activity Relationship
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Transplantation, Heterologous
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src-Family Kinases / antagonists & inhibitors*
Substances
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Enzyme Inhibitors
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Indicators and Reagents
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Nitriles
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Quinolines
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src-Family Kinases