中文摘要：

目的：获得高活性且具有抗多药耐药活性的抗肿瘤新化合物。方法：5-甲氧基吲哚与氯代物或酰氯反应得到一位氮取代的5-甲氧基吲哚。将其与草酰氯反应，再以4β-氨基-4’-去甲表鬼臼毒素为原料，经缩合反应得到目标化合物。体外活性采用Hela细胞筛选模型进行评价。结果：通过草酰桥成功将吲哚和去甲表鬼臼毒素拼接，并对吲哚一位进行改造，合成了8个新化合物。结论：合成的8个化合物中部分具有良好的抗肿瘤活性，其中化合物7a、7b的活性优于阳性对照依托伯苷。

英文摘要：

Objective： To obtain compounds with superior antitumor bioactivity and overcoming multidrug resistance. Methods： The 5- methoxyindole was reacted with alkyl chlorides or acyl chlorides to get N-substituted 5-methoxy-indoles. N-substituted 5-methoxyindol-3-ylglyoxyl chlorides were prepared by the reaction of various N-substituted 5-methoxyindoles with oxalyl chloride. Subsequently, it was coupled with 4-amino-4＇ -demethylepipodophyllotoxin in the presence of triethylamine to generate the products. HeLa cell line was used to assess the cytotoxicity of these compounds in vitro. Results： Through the oxalyl bridge indoles and success split joint podophyllotoxin, and 8 novel podophyllotoxin derivatives were synthesized. Conclusion：Part of the eight compounds which are sythesised show favourable antitumor activities, and some compounds （7a, 7b） show comparable antitumor activities to that of etoposide.