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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.
Using 18β-glycyrrhetinic acid as raw material, 18β-glycyrrhetinic acid piperazine is conveniently obtained through simple amidation reaction, and then 10 is rapidly and efficiently synthesized with carbon disulfide, potassium carbonate and halogenated hydrocarbons with different structures A new type of glycyrrhetinic acid amide derivatives containing amino dithiocarbamate structure were confirmed by IR, 1H NMR, 13C NMR and HR-MS. All the compounds were identified as tetramethylazolamide The cytotoxic activity of these compounds on human hepatocellular carcinoma cell line SMMC-7721 was evaluated by MTT assay.The results of preliminary bioassay showed that the compounds have significant inhibitory effects on the proliferation and induction of apoptosis of human hepatocellular carcinoma cells 72 h after administration, the optimal IC50 value of IC50 was only 14.42μg / mL.