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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (06): 916-923. 上一篇    下一篇

研究论文

吲哚马来酰亚胺类化合物的合成及其抗肿瘤活性

徐桂清a,b ; 胡永洲*,a; 张 冲a ; 何俏军a; 杨 波a   

  1. (a浙江大学药学院 杭州 310058)
    (b河南师范大学化学与环境科学学院 新乡 453007)
  • 收稿日期:2008-06-23 修回日期:2008-10-30 发布日期:2009-06-20
  • 通讯作者: 胡永洲

Synthesis and Antitumor Activity of Indolemalylimide Derivatives

Xu, Guiqingb; Hu, Yongzhou*,a ; Zhang, Chonga; He, Qiaojuna; Yang, Boa   

  1. (a School of Pharmaceutical Science, Zhejiang University, Hangzhou 310058)
    (b College of Chemistry and Environmental Science, Henan Normal University, Xinxiang 453007)
  • Received:2008-06-23 Revised:2008-10-30 Published:2009-06-20
  • Contact: Hu, Yongzhou

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被引次数

10

为寻找具有抗肿瘤活性的新化合物, 设计合成吲哚马来酰亚胺类化合物, 并评价其体外抗肿瘤活性. 以吲哚与2-氯乙酰胺为起始原料, 经取代、缩合等反应合成了单吲哚马来酰亚胺衍生物5a～5t, 以5-硝基吲哚和不同的N-(3-氯丙基)叔胺经取代、还原、缩合等反应得到了双吲哚马来酰亚胺衍生物9a～9f. 共合成了26个未见文献报道的新化合物, 其结构经质谱、元素分析和核磁共振氢谱确证. 采用MTT法, 测试了目标化合物对肿瘤细胞株HL60, ECA-109, A549, SMMC-7721和PC-3的增殖抑制活性, 结果表明部分化合物对所测肿瘤细胞株均显示一定的抑制作用.

关键词: 合成, 抗肿瘤活性, 吲哚马来酰亚胺

To discover novel compounds with antitumor activities, a series of indolylmaleimide derivatives were designed, synthesized and evaluated for their antitumor activities in vitro. Starting with indole and 2-chloroacetamide, followed by substitution and condensation, monoindolyl derivatives 5a～5t were syn-thesized. Starting with 5-nitroindole and different N-(3-chloropropyl)tertiary amines, followed by substitu-tion, reduction and condensation, diindolyl derivatives 9a～9f were synthesized. Twenty six novel com-pounds were synthesized, and their structures were confirmed by ESI-MS, elemental analysis and 1H NMR. The antitumor activities of the target compounds were evaluated with HL60, ECA-109, A549, SMMC-7721 and PC-3 in vitro. The in vitro antitumor activity showed that some compounds displayed inhibition to a certain degree against tested cells.

Key words: synthesis, antitumor, indolylmaleimide derivative