作为激酶抑制剂的4-苯胺基-3-氰基苯并[g]喹啉
4-Anilino-3-cyanobenzo[g]quinolines as kinase inhibitors.
作者信息
Zhang Nan, Wu Biqi, Wissner Allan, Powell Dennis W, Rabindran Sridhar K, Kohler Constance, Boschelli Frank
机构信息
Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2002 Feb 11;12(3):423-5. doi: 10.1016/s0960-894x(01)00776-4.
A series of 4-anilino-3-cyanobenzo[g]quinolines was prepared as potent kinase inhibitors. Compared with their bicyclic 4-anilino-3-cyanoquinoline analogues, the tricyclic 4-anilino-3-cyanobenzo[g]quinolines are less active against EGF-R kinase, equally active against MAPK kinase (MEK), and more active against Src kinase. For Src kinase inhibition, the best activity is obtained when both the 7- and 8-positions are substituted with alkoxy groups. Several of these kinase inhibitors show potent growth inhibitory activity in tumor cells.
制备了一系列4-苯胺基-3-氰基苯并[g]喹啉作为有效的激酶抑制剂。与它们的双环4-苯胺基-3-氰基喹啉类似物相比，三环4-苯胺基-3-氰基苯并[g]喹啉对表皮生长因子受体（EGF-R）激酶的活性较低，对丝裂原活化蛋白激酶（MEK）的活性相当，对Src激酶的活性更高。对于Src激酶抑制，当7位和8位均被烷氧基取代时可获得最佳活性。这些激酶抑制剂中的几种在肿瘤细胞中显示出有效的生长抑制活性。
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