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

Haridas B Rode; Martin L Sos; Christian Grütter; Stefanie Heynck; Jeffrey R Simard; Daniel Rauh

doi:10.1016/j.bmc.2010.11.007

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

Bioorg Med Chem. 2011 Jan 1;19(1):429-39. doi: 10.1016/j.bmc.2010.11.007. Epub 2010 Nov 10.

Authors

Haridas B Rode¹, Martin L Sos, Christian Grütter, Stefanie Heynck, Jeffrey R Simard, Daniel Rauh

Affiliation

¹ Chemical Genomics Centre of the Max Planck Society, Otto-Hahn-Strasse 15, 44227 Dortmund, Germany.

PMID: 21130659
DOI: 10.1016/j.bmc.2010.11.007

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adenosine Triphosphate / metabolism
ErbB Receptors / antagonists & inhibitors*
Humans
Isoquinolines / pharmacology*
Models, Molecular
Myosin-Light-Chain Kinase / antagonists & inhibitors*
Protein Kinase Inhibitors / pharmacology*
Structure-Activity Relationship

Substances

Isoquinolines
Protein Kinase Inhibitors
Adenosine Triphosphate
ErbB Receptors
Myosin-Light-Chain Kinase