Abstract
The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth inhibition of the two series are compared with each other and with the clinical lead EKB-569. Similar activities are observed between these two series.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology*
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Cell Line
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Cyclization
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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ErbB Receptors / antagonists & inhibitors*
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Models, Molecular
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Molecular Conformation
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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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Receptor, ErbB-2 / antagonists & inhibitors*
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Nitriles
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Quinolines
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ErbB Receptors
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Receptor, ErbB-2