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Synthesis and cytotoxicity of dihydroartemisinin ethers containing cyanoarylmethyl group
Ying Li1, Jin Ming Wu, Feng Shan
1Department of Synthetic Chemistry, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China. yli@mail.shnc.ac.cn
Bioorganic & Medicinal Chemistry
|March 5, 2003
Abstract:
A new type of ether of dihydroartemisinin containing cyano and aryl groups was prepared and tested for cytotoxicity to A549, P388, L1210 and HT29 cells using the MTT assay. 12k and 12l were the most cytotoxic compounds. 13 lacking the peroxy group showed a 1000-fold less potency than 12l. Similarly, the inactive compound 14 indicated that the position of cyano groups was also important. Flow cytometry data showed that the compounds caused an accumulation of P388 cells in the G(1)-phase of the cell cycle.