Synthesis and structure–activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors

Synthesis and structure–activity relationship of a series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitrile derivatives as EGFR inhibitors is described. Compounds 29 and 30 showed potent in vitro inhibitory activity in the enzymatic assay as well as in the functional cellular assay. They are moderately selective against other types of tyrosine kinases.

A series of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles have been synthesized and tested for EGFR inhibition. Compounds 29 and 30 showed excellent enzymatic and cellular activities against EGFR.Figure optionsDownload as PowerPoint slide