Abstract
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.
MeSH terms
-
Cell Division / drug effects
-
Cells, Cultured
-
Enzyme Inhibitors / chemical synthesis*
-
Enzyme Inhibitors / pharmacology*
-
ErbB Receptors / antagonists & inhibitors
-
Indicators and Reagents
-
Mitogen-Activated Protein Kinases / antagonists & inhibitors
-
Nitriles / chemical synthesis*
-
Nitriles / pharmacology*
-
Protein Kinase Inhibitors*
-
Quinolines / chemical synthesis*
-
Quinolines / pharmacology*
-
Structure-Activity Relationship
-
Substrate Specificity
-
src-Family Kinases / antagonists & inhibitors
Substances
-
Enzyme Inhibitors
-
Indicators and Reagents
-
Nitriles
-
Protein Kinase Inhibitors
-
Quinolines
-
ErbB Receptors
-
src-Family Kinases
-
Mitogen-Activated Protein Kinases