MEK（丝裂原活化蛋白激酶激酶）抑制剂。第2部分：4-苯胺基-3-氰基-6,7-二烷氧基喹啉的构效关系。
MEK (MAPKK) inhibitors. Part 2: structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines.
作者信息
Zhang N, Wu B, Eudy N, Wang Y, Ye F, Powell D, Wissner A, Feldberg L R, Kim S C, Mallon R, Kovacs E D, Toral-Barza L, Kohler C A
机构信息
Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2001 Jun 4;11(11):1407-10. doi: 10.1016/s0960-894x(01)00238-4.
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).
已制备出一系列4-苯胺基-3-氰基-6,7-二烷氧基喹啉，其4-苯胺基上连接有不同取代基，这些化合物是有效的MEK（丝裂原活化蛋白激酶激酶）抑制剂。当苯基或噻吩基通过疏水连接基（如氧、硫或亚甲基）连接到苯胺的对位时，可获得最佳活性。最具活性的化合物对MEK（丝裂原活化蛋白激酶激酶）表现出低纳摩尔级的IC(50)，并在LoVo细胞（人结肠肿瘤细胞系）中具有强大的生长抑制活性。
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