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.