A series of 4-aminoquinazoline derivatives were designed and synthesized as epidermal growth factor receptor (EGFR) inhibitors in our group. The bioassay results showed all the target compounds possessed potential anti-tumor activities against on A549 and H1975 cell lines. The IC50 values of 8.35 (for A549) and 19.18 μM (for H1975) exhibited remarkable inhibitory activity of compound 7d, which were better compared to the positive control Afatinib (IC50 = 10.41 μM for A549, IC50 = 24.96 μM for H1975). In addition, the molecular docking and ADME prediction of compound 7d was carried out. The experimental results show the compound 7d is worth to further research and discuss.

Liang-Liang Chi, Zhi-Qiang Cai, Bo Wang, Wei-Tao Qin, Ya-Nan Wang, Qiao-Qiao Feng and Wen-Jie Ren