Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (1): 141-148.DOI: 10.6023/cjoc201607028 Previous Articles     Next Articles


3-epi-Jaspine B类似物的合成和抗肿瘤活性评价

张恩a, 王上a, 焦伟伟a, 王铭铭a, 岳静飞a, 徐帅民a, 王亚娜a, Horst-Dieter Ambrosib, 刘宏民a   

  1. a 郑州大学药学院 新药创制与药物安全性评价河南省协同创新中心 郑州 450001;
    b AnalytiCon Discovery GmbH, Hermannswerder Haus 17, 14473 Potsdam, Germany
  • 收稿日期:2016-07-19 修回日期:2016-08-19 发布日期:2016-09-08
  • 通讯作者: 张恩, 王亚娜;
  • 基金资助:

    国家自然科学基金(No. U1204206)和河南省教育厅(No. 17A350004)资助项目.

Synthesis and Antitumor Evaluation of 3-epi-Jaspine B Analogues

Zhang Ena, Wang Shanga, Jiao Weiweia, Wang Mingminga, Yue Jingfeia, Xu Shuaimina, Wang Ya'naa, Ambrosi Horst-Dieterb, Liu Hongmina   

  1. a Collaborative Innovation Center of New Drug Research and Saftry Evaluation, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001;
    b AnalytiCon Discovery GmbH, Hermannswerder Haus 17, 14473 Potsdam, Germany
  • Received:2016-07-19 Revised:2016-08-19 Published:2016-09-08
  • Supported by:

    Project supported by the National Natural Science Foundation of China(No. U1204206) and the Education Department of Henan Province(No. 17A350004).

Jaspine B is a natural product with significant antitumor activity,which was isolated from the marine sponge Pachastrissa sp.In order to find new antitumor compounds with high efficiency and succinct synthetic methods,a series of 3-epi-jaspine B analogues were designed and synthesized.16 compounds were synthesized and all of them were unknown in the literature.Their structures were determined by 1H NMR,13C NMR and HRMS.The antitumor activity of these compounds against four tumor cell lines B16-F10,A-549,MCF-7 and PC-3 was assayed using thiazolyl blue(MTT) assay,and some compounds showed potent inhibitory effect on tumor cells.Compounds 8f and 11 were more potent against A-549 with IC50 of(9.646±0.984) and(7.144±0.854)μg/mL.

Key words: 3-epi-jaspine B, antitumor, hydrogen sulfide, analogue