Novel EGFR/HER2 inhibitors of oxazolo[4,5-g]quinazolin-2(1H)-one were synthesized.
Four compounds exhibited high inhibition against EGFR and HER2 kinase.
Comp. 12f had high inhibition against A549 and SK-Br3 cell lines.
Comp. 12f exhibited the lower toxicity against HELF cell than Lapatinib.
Comp. 12f presented higher inhibition in vivo antitumor activity than Lapatinib.