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

…, A Wissner, MB Floyd, ED Kovacs, L Toral-Barza…

Index: Zhang, Nan; Wu, Biqi; Powell, Dennis; Wissner, Allan; B. Floyd, Middleton; D. Kovacs, Eleonora; Toral-Barza, Lourdes; Kohler, Constance Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 24 p. 2825 - 2828

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Citation Number: 50

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.