熊果酸-3-取代丙醇酯衍生物的合成及抗肿瘤活性研究有机化学.pdfVIP

DOI: 10.6023/cjoc1109251 研究论文 有机化学 Chinese Journal of Organic Chemistry ARTICLE 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 (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) 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, Xiaa Bai, Xuea Wu, Kea Wang, Yujuna Shi, Wangqib Li, Ying*,a Yin, Shufan*,a (a Collage of Chemistry, Sichuan University, Chengdu 610064) b ( Sichuan 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 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. Keywords ursolic acid; 3-substituted propanolursolate; synthesis; antitumor activity 熊果酸(UA)化学名 3β-羟基-熊果-12-烯-28-酸,