Acryloylamino-salicylanilides as EGFR PTK inhibitors

A series of acryloylamino-salicylanilides were synthesized as inhibitors of EGFR PTK. A strategy of pseudo six-membered ring formed through intramolecular hydrogen bonding in salicylanilides is employed to mimic the planar pyrimidine ring of quinazoline EGFR inhibitors. Acrylamido moiety is incorporated to target the Cys-773 of EGFR specifically. Some of the obtained compounds exhibited good activity as EGFR inhibitors.

Graphical abstractA series of EGFR PTK inhibitors with an acrylamido moiety at the 4- or 5-position of salicylanilides were synthesized and tested for their inhibitory activity toward the EGFR tyrosine kinase.Figure optionsDownload full-size imageDownload as PowerPoint slide