摘要
以18β-甘草次酸为原料首先经简单酰胺化反应方便地得到18β-甘草次酸哌嗪,再与二硫化碳、碳酸钾以及不同结构卤代烃"一锅煮"法快速、高效地合成了10种含氨基二硫代甲酸酯结构的新型甘草次酸酰胺类衍生物,通过IR,1H NMR,13C NMR和HR-MS对所有新化合物进行了结构确证;并以四甲基偶氮唑盐比色法(MTT)法评价了该类化合物对人肝癌细胞株SMMC-7721的细胞毒活性.初步生物活性研究结果表明,该类化合物具有明显的抑制人肝癌细胞增殖、诱导其凋亡的细胞毒活性,给药72 h,半抑制浓度IC50最优值仅为14.42μg/mL.
Ten new 18β-glycyrrhetinic acid derivatives with dithiocarbamate units were prepared by amida- tion of 18β-glycyrrhetinic acid and piperazine followed with one-pot condensation of the amide, CS2 and alkyl halides in the presence of potassium carbonate in CHCl3. The structures of all the new compounds were identified by NMR spectra, IR and HRMS technology. Anti-tumor activities of the 18β-glycyrrhetinic acid derivatives against human hepatoma SMMC-7721 cell lines were evaluated by 3-（4,5-dimethylthiazol- 2-yl）-2,5-diphenyltetrazolium bromide （MTT） method. They were found to inhibit the liver cancer cell proliferation and induce apoptosis as the lowest IC50 value was only 14.42 μg/mL.
出处
《化学学报》
SCIE
CAS
CSCD
北大核心
2012年第7期852-858,共7页
Acta Chimica Sinica
基金
国家自然科学基金(No.21062014)
教育部科学技术研究重点项目(No.210237)
宁夏自然科学基金(No.NZ0606)
云南大学自然资源药物化学教育部重点实验室开放基金(No.200902205)资助项目~~
