Among them, Compound 6a showed good inhibitory activity against EGFR mutant cells with an IC value of 0.0022 ± 0.001 μM and was approximately 1730-fold less potent against EGFR WT cells (IC: 4.499 ± 0.057 μM)...Additionally, in vivo studies confirmed that 6a suppressed tumor growth in an H1975 xenograft model (25 mg/kg/d, TGI: 90.24%). Overall, these results suggest that 6a could be a promising lead compound for overcoming the clinical EGFR T790M resistance of patients with non-small-cell lung cancers (NSCLCs).