以邻羟基萘甲醛和乙酰乙酸乙酯为原料,六氢吡啶为催化剂,通过Knoevenagel反应,利用研磨法制得3-乙酰基-5,6-苯并香豆素(A);A与4-甲氧基苯甲醛(B)和醋酸铵经一锅法合成新化合物4-(4-甲氧基苯基)-2, 6-双(5,6-苯并香豆素-3-基)吡啶(C),其结构经1H NMR,IR和元素分析表征.对反应条件进行了优化,并采用MTT法研究了化合物C对人体宫颈癌HeLa 229肿瘤细胞株的抑制作用.结果表明:当C浓度为80 μmol·L-1,作用时间为48 h时,抑制率为66.65%,IC50为45.75 μmol·L-1,与依托泊苷(IC50=42 μmol·L-1)相当.%3-Acetyl-5,6-benzocoumarin(A) was synthesized by Knoevenagel addition in piperidine, using o-hydroxy naphthaldehyde and ethyl acetoacetate as raw materials by grinding method. The novel compound,4-(4-methoxypheny)-2,6-bis(5,6-benzocoumarin-3-yl)pyridine(C) was synthesized u-sing 3-acetyl-5,6-benzocoumarin(A),4-methoxybenzaldehyde(B)and ammonium acetate as the mate-rials by one pot method. The structure was characterized by 1H NMR,IR and elemental analysis. The reaction conditions were optimized. The antitumor activities of C against human cervical cancer cell lines(Hela 229) were determined by MTT method. The results indicated that the best anti-tumor effect of C was 66.65% when the concentration was 80 μmol·L-1, and the duration was 48h, IC50was 45.75 μmol·L-1,which were equivalent to Etoposide(42 μmol·L-1).
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