Abstract: OBJECTIVE To design and synthesize a series of ferulic acid derivatives containing quinazoline structure, and to study their antitumor activity. METHODS Based on the principle of splicing, ferulic acid was combined with quinazoline, and the 6-position of quinazoline was modified to obtain the target compound. The anti-tumor activity of the target compound against lung cancer cell A549 was tested by CCK-8 method. Molecular docking technology was used to simulate the binding mode of the target compound and epidermal growth factor receptor. RESULTS The structure of the target compound was confirmed by HRMS (ESI) and ¹H-NMR. The in vitro antitumor activity results showed that the IC₅₀ of compounds 11d, 11f, 12d and 12g were lower than the positive drug of gefitinib, and the IC₅₀ of 11c was comparable to gefitinib. CONCLUSION Compound 11d (IC₅₀=3.09μmol·L^-1) has strong antitumor activity against lung cancer cell A549, which is worthy of further study.