摘要
以DMSO为溶剂,5-氟脲嘧啶(5-Fu)为修饰物,对去甲斑蝥素(2)酸酐环部分进行结构修饰,合成了一个新型的去甲斑蝥素羧酸衍生物(3),其结构经1H NMR和IR表征。采用L9(34)正交试验考察了原料比,反应温度,反应时间及溶剂用量对反应的影响。结果表明,在最佳反应条件[2 0.5 mmol,n(2)∶n(5-Fu)=1.2,于140℃反应6 h,DMSO用量15 mL]下制备的3收率为78.2%。采用MTT法研究了体外3对人肝癌细胞HepG2的抑制活性。结果表明,3在用药量为250μmol·L-1时对HepG2的抑制率为89.5%,其IC50为232.4μmol·L-1。
A novel cantharidin carboxylic derivative（3） was synthesized by structural modification of norcantharidin（2） using 5-fluorouracil（5-Fu） as the modifier in DMSO.The structure was characterized by 1H NMR and IR.The effect of material ratio,reaction temperature,reaction time and solvent amount on reaction were investigated by L9 （34） orthogonal experiment.The yield of 3 was 78.2％ under the optimum reaction conditions[2 was 0.5 mmol,n（2） ∶ n（5-Fu） was 1.2,DMSO was 15 mL,at 140 ℃ for 6 h].Antitumor activity of 3 was tested by MTT method.The results indicated that 3 exhibited good inhibition to HepG2 human cancer cells.Inhibition rate of 3 was 89.5％ at 250 μmol · L-1,and IC50 was 232.4μmol · L-1.
出处
《合成化学》
CAS
CSCD
北大核心
2013年第5期518-521,共4页
Chinese Journal of Synthetic Chemistry
基金
康缘中医药科技创新基金资助项目(HZ1006KY)
