4-Anilino-3-cyanobenzo[g]quinolines as Kinase Inhibitors
摘要:
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. (C) 2002 Elsevier Science Ltd. All rights reserved.
4-Anilino-3-cyanobenzo[g]quinolines as Kinase Inhibitors
摘要:
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. (C) 2002 Elsevier Science Ltd. All rights reserved.
This invention provides compounds of formula 1, having the structure
1
which are useful as inhibitors of protein tyro sine kinase and are antiproliferative agents.
这项发明提供了具有结构1的化合物,这些化合物可作为蛋白酪氨酸激酶的抑制剂,是抗增殖剂。
[EN] TRICYCLIC PROTEIN KINASE INHIBITORS<br/>[FR] INHIBITEURS TRICYCLIQUES DE PROTEINE KINASE
申请人:AMERICAN HOME PROD
公开号:WO2001047892A1
公开(公告)日:2001-07-05
This invention provides compounds of formula (1) which are useful as inhibitors of protein tyrosine kinase and are antiproliferative agents.