Antitumor activity and mechanisms of dual EGFR/DNA-targeting strategy for the treatment of lung cancer with EGFRL858R/T790M mutation

•Fifteen 4-anilinoquinazoline derivatives bearing nitrogen mustard or hemi mustard moieties were reported.•6g displayed the superior antiproliferative activity against H1975 cells with IC50 value of 1.45 μM.•6g could significantly inhibit the phosphorylation of EGFR and cause DNA damage.•6g efficiently inhibited tumor growth in the H1975 xenograft model without side effects.