Design, Synthesis and Antitumor Activity of Novel Artemisinin Derivatives Using Hybrid Approach

作者：Xie, Lijun; Zhai, Xin; Ren, Lixiang; Meng, Haiyan; Liu, Chun; Zhu, Wufu; Zhao, Yanfang^*

来源：Chemical & Pharmaceutical Bulletin, 2011, 59(8): 984-990.

DOI：10.1248/cpb.59.984

• artemisinin
• chalcone
• hybrid approach
• anti-tumor activity
• X-ray crystallography

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 0.85 mu m.

• 出版日期2011-8
• 单位沈阳药科大学