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有机化学
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有机化学 ›› 2011, Vol. 31 ›› Issue (07): 1122-1126. 上一篇    下一篇

研究简报

两类氮芥衍生物的合成及其生理活性研究

许凤华1,2，甘莹2，张亚宏2，罗稳2，马红霞2，王超杰2，赵瑾*,1,2   

  1. (1河南大学化学化工学院 开封 475004)
    (2河南省天然药物与免疫工程重点实验室 开封 475004)
  • 收稿日期:2010-09-17 修回日期:2011-01-12 发布日期:2011-02-25
  • 通讯作者: 赵瑾 E-mail:zhaojin@henu.edu.cn

Synthesis and Biological Activity of Two Kinds of Nitrogen Mustard Derivatives

Xu, Fenghuaa,b Gan, Yingb Zhang, Ya-hongb Luo, Wenb
Ma, Hongxiab Wang, Chaojieb Zhao, Jin*,a,b   

  1. (1 College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475004)
    (2 Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Prov-ince, Henan University, Kaifeng 475004)
  • Received:2010-09-17 Revised:2011-01-12 Published:2011-02-25

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被引次数

8 | 1

设计合成了3个苯胺氮芥和6个萘酰亚胺-氮芥衍生物, 产物结构均经1H NMR, 13C NMR, ESI-MS和元素分析确认. 使用MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide]法测试了9个化合物对HL-60, K562 和SMMC-7721三种肿瘤细胞的体外抗肿瘤活性, 测试结果表明所有目标化合物对HL-60细胞均具有较好的体外活性, 其中化合物5活性优于商品药物美法仑. 正常细胞和肿瘤细胞的选择性测试表明, 5a对SMMC-7721细胞有较好的选择性, 且优于阳性对照物美法仑.

关键词: 氮芥衍生物, 合成, 生理活性

Three aniline nitrogen mustard and six naphthalimide-nitrogen mustard derivatives were designed and synthesized. The structures of the synthesized compounds were confirmed by 1H NMR, 13C NMR, ESI-MS techniques and elemental analysis. The prelimilary antitumor activity was evaluated on HL-60, K562 and SMMC-7721 cell lines by MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. The results demonstrated that target compounds exhibited antitumor activity for HL-60 and the activity of compound 5 was superior to commercial drug melphalan. Besides, the activity of compound 5a against SMMC-7721 cells is more selectivity than that of QSG-7701 cell lines.

Key words: nitrogen mustard derivative, synthesis, biological activity