Abstract
Neutral 5-substituted 4-anilinoquinazolines addressed high in vivo clearance and phospholipidosis associated with previous basic compounds. A representative compound 8a inhibited tumor growth in a mouse xenograft model when co-administered with the cytochrome P450 inhibitor 1-aminobenzotriazole (ABT), and data are consistent with pharmacology primarily reflecting inhibition of erbB2 receptor tyrosine kinase.
MeSH terms
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Administration, Oral
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Aniline Compounds / chemistry
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Animals
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / pharmacology*
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Antineoplastic Combined Chemotherapy Protocols
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Cell Proliferation / drug effects
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Dogs
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Drug Synergism
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Mice
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Molecular Structure
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Neoplasms / drug therapy*
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Quinazolines / chemistry*
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Quinazolines / pharmacokinetics
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Quinazolines / pharmacology*
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Rats
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Receptor, ErbB-2 / antagonists & inhibitors*
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Triazoles / pharmacology
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Xenograft Model Antitumor Assays
Substances
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Aniline Compounds
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Antineoplastic Agents
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Quinazolines
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Triazoles
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1-aminobenzotriazole
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Receptor, ErbB-2
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aniline