Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase and epidermal growth factor receptor.
Here we present the synthesis and biological activity of a series of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase (MLCK) and the epidermal growth factor receptor kinase (EGFR). The inhibitory effect of these molecules was found to be dependent on the nature of the substituents at the 7-position of the isoquinoline scaffold.
Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, 44227 Dortmund, Germany.
Haridas B
HB
Rode
Martin L
ML
Sos
Christian
C
Grütter
Stefanie
S
Heynck
Jeffrey R
JR
Simard
Daniel
D
Rauh
D000255:Adenosine Triphosphate / Q000378:metabolism; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D006801:Humans; D007546:Isoquinolines / Q000494:pharmacology*; D008958:Models, Molecular; D009219:Myosin-Light-Chain Kinase / Q000037:antagonists & inhibitors*; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D007546:Isoquinolines; D047428:Protein Kinase Inhibitors; D000255:Adenosine Triphosphate; D066246:ErbB Receptors; D009219:Myosin-Light-Chain Kinase