Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (5): 1097-1103.DOI: 10.6023/cjoc201409039 Previous Articles     Next Articles



魏梦雪a, 徐建a, 张和a, 李学强a,b   

  1. a 宁夏大学化学化工学院 银川 750021;
    b 宁夏天然药物工程技术研究中心 银川 750021
  • 收稿日期:2014-09-24 修回日期:2014-10-28 发布日期:2015-01-28
  • 通讯作者: 李学强
  • 基金资助:


Synthesis and Anti-tumor Effect of Artemisone Derivatives

Wei Mengxuea, Xu Jiana, Zhang Hea, Li Xueqianga,b   

  1. a School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan 750021;
    b Ningxia Engineering Research Center for Natural Medicines, Yinchuan 750021
  • Received:2014-09-24 Revised:2014-10-28 Published:2015-01-28
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos.21462032, 21062014) and the Research Starting Funds for Imported Talents of Ningxia University (No.80020241).

The artemisone was rationally designed to be attached with an ester unit, and a series of such artemisone derivatives were practically prepared from dihydroartemisinin. The synthetic route was combined with amination, oxidation, alkylation and esterification. All the new artemisone derivatives were identified by NMR, IR and HRMS technology. The anti-tumor activities of artemisone derivatives against human hepatoma SMMC-7721 cell lines were evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric method. It revealed that they could obviously exert their inhibition of proliferation of the liver cancer cells by inducing apoptosis. Compound 7b exhibited the most potent antiproliferative activity with IC50 value of 0.06 μmol/L treatment for 72 h. Compared with artemisinin, dihydroartemisinin and artemisone, the new artemisone derivatives are superior to each of them in antitumor activity. These results are significant to the potential application of artemisone derivatives in the further development of new anticancer drugs.

Key words: artemisinin, artemisone, esters, synthesis, anti-tumor activity