Abstract
A series of novel pyrrolopyridazine derivatives have been discovered to be HER-2 inhibitors. These compounds selectively inhibited HER-2 kinase activity at low nanomolar concentrations. Compound 7d was identified as a potent HER-2 inhibitor with an IC(50) of 4 nM.
MeSH terms
-
Drug Design
-
Enzyme Inhibitors / chemical synthesis
-
Enzyme Inhibitors / pharmacology*
-
Models, Molecular
-
Pyridazines / chemical synthesis
-
Pyridazines / pharmacology*
-
Pyrroles / chemical synthesis
-
Pyrroles / pharmacology*
-
Structure-Activity Relationship
-
TYK2 Kinase / antagonists & inhibitors*
-
TYK2 Kinase / metabolism
Substances
-
Enzyme Inhibitors
-
Pyridazines
-
Pyrroles
-
Pyrrolopyridazine
-
TYK2 Kinase