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ID: ALA1134081
Journal: Bioorg Med Chem Lett
Title: MEK (MAPKK) inhibitors. Part 2: structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines.
Authors: Zhang N, Wu B, Eudy N, Wang Y, Ye F, Powell D, Wissner A, Feldberg LR, Kim SC, Mallon R, Kovacs ED, Toral-Barza L, Kohler CA.
Abstract: A series of 4-anilino-3-cyano-6,7-dialkoxyquinolines with different substituents attached to the 4-anilino group has been prepared that are potent MEK (MAP kinase kinase) inhibitors. The best activity is obtained when a phenyl or a thienyl group is attached to the para-position of the aniline through a hydrophobic linker, such as an oxygen, a sulfur, or a methylene group. The most active compounds show low nanomolar IC(50)'s against MEK (MAP kinase kinase), and have potent growth inhibitory activity in LoVo cells (human colon tumor line).
CiteXplore: 11378365