有机化学 ›› 2008, Vol. 28 ›› Issue (12): 2107-2114. 上一篇    下一篇

研究论文

二苯丁脂类木脂素及衍生物的合成和抗肿瘤活性研究

夏亚穆*,a ; 赫 蕊b; 丁一宁a   

  1. (a青岛科技大学化工学院 青岛 266042)
    (b青岛科技大学数理学院 青岛 266042)
  • 收稿日期:2008-03-27 修回日期:2008-06-13 发布日期:2008-12-28
  • 通讯作者: 夏亚穆

Synthesis and Anti-tumoractivities of Dibenzylbutylester Lignans and Their Analogues

XIA, Ya-Mu*,a ; HE, Ruib; DING, Yi-Ninga   

  1. (a College of Chemical Engineering, Qingdao University of Science and Technology, Qingdao 266042)
    (b College of Mathematics and Physics, Qingdao University of Science and Technology, Qingdao 266042)
  • Received:2008-03-27 Revised:2008-06-13 Published:2008-12-28
  • Contact: XIA, Ya-Mu

以胡椒醛和藜芦醛为原料, 通过Stobbe缩合和烷基化反应构建木脂素骨架、手性试剂拆分, 经官能团转换后, 得到了10个二苯丁脂类木脂素, 其中4个为天然产物. 合成得到的化合物进行了抗肿瘤活性测定, 结果表明, 部分化合物物具有较强的抑制乳腺癌细胞活性.

关键词: 二苯丁脂类木脂素, 合成, 抗肿瘤活性

A useful synthetic route to dibenzylbutylester lignans was described using piperonal and veratraldehyde as the starting materials. This method involves Stobbe condensation and alkylation reactions to give the skeleton of lignan, then fellowed by transformation of functional groups to get target compounds. By this route, ten dibenzylbutylester lignans were obtained, four of which were natural products. The products were tested against human tumors, and some compounds show better activity against breast cancer cells.

Key words: synthesis, dibenzylbutylester lignan, antitumor activity