Abstract
A series of 3-cyano-4-(phenoxyanilino)cyanoquinolines has been prepared as MEK (MAP kinase kinase) inhibitors. The best activity is seen with alkoxy groups at both the 6- and 7-positions. The lead compounds show low nanomolar IC50's against MAP kinase kinase, and have potent inhibitory activity in tumor cells.
MeSH terms
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Aniline Compounds / chemical synthesis
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Aniline Compounds / pharmacology
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Cell Division / drug effects
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Colonic Neoplasms / pathology
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Enzyme-Linked Immunosorbent Assay
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Humans
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Inhibitory Concentration 50
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Mitogen-Activated Protein Kinase Kinases / antagonists & inhibitors*
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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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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Aniline Compounds
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Antineoplastic Agents
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Nitriles
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Quinolines
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Mitogen-Activated Protein Kinase Kinases