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熊果酸-3’-取代丙醇酯衍生物的合成及抗肿瘤活性研究
引用本文:李霞,白雪,吴科,王裕军,石万棋,李颖,尹述凡.熊果酸-3’-取代丙醇酯衍生物的合成及抗肿瘤活性研究[J].有机化学,2012(4):703-708.
作者姓名:李霞  白雪  吴科  王裕军  石万棋  李颖  尹述凡
作者单位:1. 四川大学化学学院 成都610064
2. 四川国康药业有限公司 成都610041
摘    要: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

Synthesis and Antitumor Activities of 3(')-Substituted Propanolursolates
Li, Xia , Bai, Xue , Wu, Ke , Wang, Yujun , Shi, Wangqi , Li, Ying , Yin, Shufan.Synthesis and Antitumor Activities of 3(')-Substituted Propanolursolates[J].Chinese Journal of Organic Chemistry,2012(4):703-708.
Authors:Li  Xia  Bai  Xue  Wu  Ke  Wang  Yujun  Shi  Wangqi  Li  Ying  Yin  Shufan
Affiliation:Li,Xiaa Bai,Xuea Wu,Kea Wang,Yujuna Shi,Wangqib Li,Ying,a Yin,Shufan,a(aCollage of Chemistry,Sichuan University,Chengdu 610064)(bSichuan Guokang Pharmaceutical Co.,Ltd,Chengdu 610041)
Abstract: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 of1H 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.
Keywords:ursolic acid  3’-substituted propanolursolate  synthesis  antitumor activity
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