Chemical and Pharmaceutical Bulletin p. 984 - 990 (2011)
Update date:2022-08-04
Topics:
Xie, Lijun
Zhai, Xin
Ren, Lixiang
Meng, Haiyan
Liu, Chun
Zhu, Wufu
Zhao, Yanfang
In an attempt to develop potent and selective anti-tumor agents, two novel series of artemisinin-chalcone hybrids were designed, synthesized and screened for their antitumor activities against HT-29, A549, MDA-MB-231, HeLa and H460 cell lines in vitro. Nearly all of the tested compounds showed significantly increased anti-tumor activity compared with the corresponding dihydroartemisinin (DHA). Most of the title compounds displayed good selectivity toward HT-29 and HeLa cell lines with IC50 values ranging from 0.09 to 0.85μM. Among them, the most promising compound 9c (IC50 range of 0.09-0.93μM) was 10.5- to 70-times more active than DHA (IC50 range of 5.6-15.6μM) respectively.
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