Author/Authors :
Nan Zhang، نويسنده , , Biqi Wu، نويسنده , , Nancy Eudy، نويسنده , , Yanong Wang، نويسنده , , Fei Ye، نويسنده , , Dennis Powell، نويسنده , , Allan Wissner، نويسنده , , Larry R. Feldberg، نويسنده , , Steven C. Kim، نويسنده , , Robert Mallon، نويسنده , , Eleonora D. Kovacs، نويسنده , , Lourdes Toral-Barza، نويسنده , , Constance A. Kohler، نويسنده ,
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 IC50ʹs against MEK (MAP kinase kinase), and have potent growth inhibitory activity in LoVo cells (human colon tumor line).
