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有机化学
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有机化学 ›› 2012, Vol. 32 ›› Issue (04): 703-708.DOI: 10.6023/cjoc1109251 上一篇    下一篇

研究论文

熊果酸-3'-取代丙醇酯衍生物的合成及抗肿瘤活性研究

李霞a, 白雪a, 吴科a, 王裕军a, 石万棋b, 李颖a, 尹述凡a   

  1. a 四川大学化学学院 成都 610064;
    b 四川国康药业有限公司 成都 610041
  • 收稿日期:2011-09-25 修回日期:2011-11-29 发布日期:2012-04-24
  • 通讯作者: 李 颖, 尹述凡 E-mail:chuandayouji217@163.com

Synthesis and Antitumor Activities of 3'-Substituted Propanolursolates

Li Xiaa, Bai Xuea, Wu Kea, Wang Yujuna, Shi Wangqib, Li Yinga, Yin Shufana   

  1. a Collage of Chemistry, Sichuan University, Chengdu 610064;
    b Sichuan Guokang Pharmaceutical Co., Ltd, Chengdu 610041
  • Received:2011-09-25 Revised:2011-11-29 Published:2012-04-24

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被引次数

9 | 1

熊果酸与1,3-二溴丙烷反应制得中间体熊果酸-3'-溴代丙醇酯(1), 含溴醇酯1 与含氮化合物反应, 合成了系列熊果酸含氮衍生物2a～2j, 均未见文献报道, 其结构经1H NMR, 13C NMR, IR, MS 确认. 初步的抗肿瘤生物活性研究表明, 部分化合物的抗肿瘤活性与熊果酸相比均有提高, 其中化合物2e 具有更强的抑制活性.

关键词: 熊果酸, 3'-溴代丙醇酯, 合成, 抗肿瘤

3'-Substituted propanolursolates (1) were obtained by a reaction of ursolic acid with trimethylene bromide. This intermediate reacted with several N-containing compounds to afford a series of new derivatives 2a～2j. The structures of new products were characterized by means of 1H NMR, 13C NMR, IR and MS techniques. The preliminary bioassay test shows that several compounds give a good antitumor activity, and most of them are better than that of parent ursolic acid. Among them, compound 2e shows the best activity.

Key words: ursolic acid, 3'-substituted propanolursolate, synthesis, antitumor activity