1345891-24-8Relevant articles and documents
The application of tandem aza-wittig reaction to synthesize artemisinin-guanidine hybrids and their anti-tumor activity
Xie, Lijun,Zhao, Yanfang,Zhai, Xin,Li, Peng,Liu, Chun,Li, Yangxiong,Gong, Ping
, p. 631 - 638 (2011)
Three series of novel artemisinin-guanidine hybrids 4a-4f, 8a-8h and 9a-9h have been facilely synthesized via four-component reaction (aza-Wittig reaction) and evaluated for their anti-tumor activities against A549, HT-29 and MDA-MB-231 cell lines in vitro. All of the tested compounds showed enhanced anti-tumor activities with IC50 values ranging from 0.02 μM to 12.0 μM as compared to DHA (dihydroartemisinin). Among them, artemisinin derived dimers, compounds 9b (IC50 = 0.05 μM), 9d (IC50 = 0.06 μM) and 9f (IC50 = 0.02 μM) were found to be most active against HT29 cells. An efficient method to generate three series of novel artemisinin derivates using multi-component reaction was developed. From the preliminary results we can conclude that artemisinin guanidine hybrids may be promising candidates for new anticancer agents. Copyright