Nancy H. Eudy

MEK (MAPKK) inhibitors. Part 2: structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines.

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).

4H-1,4-benzothiazine derivatives via a novel lead tetraacetate induced ring contraction.

Abstract 8-Chloro-3,4-dihydro-5-(2-thienyl)-2H-1,6-benzothiazocine underwent a facile lead tetraacetate induced ring contraction forming several 3-(2-thienyl)-4H-1,4-benzothiazine derivatives.