Synthesis and Anticancer Activities of Novel Piperazine-Aliphatic Amide Derivatives Containing Dihydroartemisinin
WEI Meng-xue1a，1b, MA Chao1a, XU Jian1a, ZHANG He1a, LI Xue-qiang1a，1b
a. School of Chemistry and Chemical Engineering; b. Ningxia Engineering Research Center for Natural Medicines, 1. Ningxia University, Yinchuan 750021, China
Abstract：A piperazine-amide derivative(2) was obtained by one-pot method, using dihydroartemisinin（DHA）, oxalyl chloride and piperazine as materials. Six novel piperazine-aliphatic amide derivatives（4a～4f） were synthesized by acylation of 2 with aliphatic acyl chloride．The structures were characterized by 1H NMR, 13C NMR, IR and HR-ESI-MS. The anti-cancer activities in vitro of 4a~4f against human hepatoma SMMC-7721 cell lines were investigated by MTT method. The preliminary bioassay results showed that 4a～4f inhibited the proliferation and induced the apoptosis of SMMC-7721. Especially dihydroartemisinin piperazinechlorine acetamide（4c)had the best inhibition activity against SMMC-7721 with IC50 0.05 μM, which was superior to artemisinin（IC50 0.53 μM） and DHA（IC50 0.52 μM）.
2015, Vol. 23 
