Chinese Journal of Organic Chemistry >
Synthesis and Anti-tumor Effect of Artemisone Derivatives
Received date: 2014-09-24
Revised date: 2014-10-28
Online 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
Wei Mengxue , Xu Jian , Zhang He , Li Xueqiang . Synthesis and Anti-tumor Effect of Artemisone Derivatives[J]. Chinese Journal of Organic Chemistry, 2015 , 35(5) : 1097 -1103 . DOI: 10.6023/cjoc201409039
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