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有机化学
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有机化学 ›› 2014, Vol. 34 ›› Issue (6): 1167-1171.DOI: 10.6023/cjoc201312029 上一篇    下一篇

研究论文

鬼臼毒素五元氮杂环类衍生物的合成及细胞毒活性研究

朱培芳a, 赵静峰b, 羊晓东b, 张洪彬b   

  1. a. 云南中医学院实验中心 昆明 650500;
    b. 云南大学教育部自然资源药物化学重点实验室 昆明 650091
  • 收稿日期:2013-12-24 修回日期:2014-01-27 发布日期:2014-02-14
  • 通讯作者: 赵静峰 E-mail:jfzhao@ynu.edu.cn
  • 基金资助:
    国家自然科学基金（Nos. 20702045，21072164）和云南省自然科学基金（Nos. 2013FA028，2012FB113）资助项目.

Synthesis and Cytotoxic Activity of Podophyllotoxin Five-Membered N-Heterocyclic Derivatives

Zhu Peifanga, Zhao Jingfengb, Yang Xiaodongb, Zhang Hongbinb   

  1. a. Experimental Center, Yunnan University of Traditional Chinese Medicine, Kunming 650500;
    b. Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of Education, Yunnan University, Kunming 650091
  • Received:2013-12-24 Revised:2014-01-27 Published:2014-02-14
  • Supported by:
    Project supported by the National Natural Science Foundation of China (Nos. 20702045, 21072164) and the Natural Science Foundation of Yunnan Province (Nos. 2013FA028, 2012FB113).

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被引次数

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从鬼臼毒素出发，通过简洁的合成路线合成了9个新型的鬼臼毒素五元氮杂环类衍生物，其结构经1H NMR，13C NMR，IR，HR-ESI-MS以及X单晶衍射确定. 对合成的新化合物进行了体外抗肿瘤活性的筛选，结果表明，化合物10具有较好的细胞毒活性，IC50值为2.63～4.73 μmol/L，对4种细胞株的活性均优于顺铂，可以作为先导化合物作进一步的结构修饰和更深入的活性研究.

关键词: 鬼臼毒素, 五元氮杂环, 结构改造, 细胞毒活性

Nine novel podophyllotoxin five-membered N-heterocyclic derivatives have been prepared from commercially podophyllotoxin. Their structures were confirmed by 1H NMR, 13C NMR, IR, HR-ESI-MS and X-ray crystallographic analysis. These derivatives have been evaluated in vitro against a panel of human tumor cell lines. Compound 10 (IC50: 2.63～4.73 μmol/L) showed superior cytotoxic activity compared with DDP (a clinically available anticancer drug) in four human tumor cell lines investigation, which is to be a lead compound for further structural modifications and activity research.

Key words: podophyllotoxin, five-membered N-heterocycles, structure modification, cytotoxic activity