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.
韩春, 吴林韬, 苏峰, 胡晓琴, 王晓霞, 李梦瑶, 武曦, 孙龙. 香豆素-苯胺嘧啶拼合物的合成及抗非小细胞肺癌活性[J]. 中国药学杂志, 2020, 55(3): 177-182.
HAN Chun, WU Lin-tao, SU Feng, HU Xiao-qin, WANG Xiao-xia, LI Meng-yao, WU Xi, SUN Long. Synthesis and Anti-NSCLC Activity of Coumarin-anilinopyrimidine Combined Compounds. Chinese Pharmaceutical Journal, 2020, 55(3): 177-182.
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