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Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of MLCK and EGFR

Literature Life Science

Identify novel inhibitors of MLCK,by detecting substrate phosphorylation using HTRF as a readout

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.

Details

Bioorg Med Chem. 2011;19(1):429-39.

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