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Bioorg Med Chem Lett. 2000 Dec 18;10(24):2825-8.

Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors.

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  • 1Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA.


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.

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