Abstract
We describe the identification of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine (3), a potent, orally active Src inhibitor with desirable PK properties, demonstrated activity in human tumor cell lines and in animal models of tumor growth.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cytochrome P-450 Enzyme Inhibitors
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Dogs
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacokinetics
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Enzyme Inhibitors / pharmacology*
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Half-Life
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Humans
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Isoenzymes / antagonists & inhibitors
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Lung Neoplasms / drug therapy
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Mice
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Mice, Nude
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Models, Molecular
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Molecular Conformation
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Neoplasm Transplantation
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Protein Binding
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Pyrrolidines / chemical synthesis*
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Pyrrolidines / pharmacology
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Rats
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Structure-Activity Relationship
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Triazines / chemical synthesis*
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Triazines / pharmacology
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src-Family Kinases / antagonists & inhibitors*
Substances
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(7-(2,6-dichlorophenyl)-5-methylbenzo(1,2,4)triazin-3-yl)-(4-(2-pyrrolidin-1-ylethoxy)phenyl)amine
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Antineoplastic Agents
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Cytochrome P-450 Enzyme Inhibitors
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Enzyme Inhibitors
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Isoenzymes
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Pyrrolidines
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Triazines
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src-Family Kinases