ABSTRACT
OBJECTIVE: To design and synthesize a series of combined compounds of coumarins and anilinopyrimidines (7a-7j) investigate their anti-NSCLC activities in vitro. METHODS: The target compounds were obtained by condensation of anilinopyrimidines and coumarin derivatives via the combination principle, then the anti-NSCLC activity of these compounds was studied by MTT. Molecular docking studies were performed to afford the binding mode of the compound and EGFR. RESULTS: The structures of the target compounds were confirmed by MS, 1H-NMR and 13C-NMR. Compounds 7a-7j displayed different degrees of inhibitory activities on the proliferation of NSCLC cell line H1975 (IC50=2.70-17.59 μmol•L-1). Six compounds showed higher anti-proliferative activity on H1975 cells than gefitinib (IC50=9.18 μmol•L-1). CONCLUSION: Compound 7j (IC50=2.70 μmol•L-1) has the best inhibitory effect on H1975 cells, suggesting that 7j may be a potential anti-NSCLC agent for further investigation.