A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: Design, synthesis, and biological activity

A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine was synthesized and found to have potent dual EGFR/HER2 kinase inhibitory activity. The structure-based drug design of this molecule as well as the kinase and cellular inhibition of HER2 kinase dependent cell lines will be discussed.

Graphical abstractA novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine 11 was synthesized and found to have potent dual EGFR/HER2 kinase inhibitory activity. The design, synthesis, and proposed binding conformation of 11 in EGFR kinase is described.Figure optionsDownload full-size imageDownload as PowerPoint slide