Acta Chimica Sinica ›› 2012, Vol. 70 ›› Issue (07): 852-858 .DOI: 10.6023/A1111051 Previous Articles     Next Articles

Full Papers

新型18β-甘草次酸氨基二硫代甲酸酯衍生物的合成及抗癌活性研究

陈凑喜a, 李学强a,b, 李天才a, 周学章c   

  1. a 宁夏大学化学化工学院 银川 750021;
    b 宁夏天然药物工程技术研究中心 银川 750021;
    c 宁夏大学 西部特色生物资源保护与利用教育部重点实验室 银川 750021
  • 收稿日期:2011-11-05 修回日期:2012-01-31 出版日期:2012-04-14 发布日期:2012-02-14
  • 通讯作者: 李学强 E-mail:lixq@nxu.edu.cn
  • 基金资助:

    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)和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.

Synthesis and Anti-tumor Activities of Novel 18β-Glycyrrhetinic Acid Derivatives Attaching Dithiocarbamate Units

Chen Couxia, Li Xueqianga,b, Li Tiancaia, Zhou Xuezhangc   

  1. a School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan 750021;
    b Ningxia Development Center of Natural Products and Medication, Yinchuan 750021;
    c Key Laboratory of Ministry of Education for Protection and Utilization of Special Biological Resources in Western China, Ningxia University, Yinchuan 750021
  • Received:2011-11-05 Revised:2012-01-31 Online:2012-04-14 Published:2012-02-14
  • Supported by:

    Project supported by National Natural Science Foundation of China (No. 21062014), Key Project of Chinese Ministry of Education (No. 210237), Natural Science Foundation of Ningxia Province of China (No. NZ0606) and Key Laboratory of Medicinal Chemistry for Natural Resource, Yunnan University (No. 200902205) for financial support.

Ten new 18β-glycyrrhetinic acid derivatives with dithiocarbamate units were prepared by amidation 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.

Key words: 18β-glycyrrhetinic acid, dithiocarbamates, synthesis, anti-tumor activity