Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (3): 731-738.DOI: 10.6023/cjoc201610017 Previous Articles     Next Articles



刘娟娟a, 卢言菊a,b, 王婧a,b, 毕良武a,b, 赵振东a,b   

  1. a 中国林业科学研究院林产化学工业研究所 生物质化学利用国家工程实验室 国家林业局林产化学工程重点开放性实验室 江苏省生物质能源与材料重点实验室 南京 210042;
    b 中国林业科学研究院林业新技术研究所 北京 100091
  • 收稿日期:2016-10-12 修回日期:2016-12-07 发布日期:2016-12-21
  • 通讯作者: 赵振东,
  • 基金资助:


Synthesis and Bioactivity Evaluation of Acylthiourea Derivatives Based on Isopimaric Acid

Liu Juanjuana, Lu Yanjua,b, Wang Jinga,b, Bi Liangwua,b, Zhao Zhendonga,b   

  1. a Institute of Chemical Industry of Forest Product, Chinese Academy of Forestry, National Engineering Laboratory for Biomass Chemical Utilization, Key and Open Laboratory on Forest Chemical Engineering State Forestry Adminstration, Key Laboratory of Biomass Energy and Material, Nanjing 210042;
    b Research Institute of Forestry New Technology, Chinese Academy of Forestry, Beijing 100091
  • Received:2016-10-12 Revised:2016-12-07 Published:2016-12-21
  • Contact: 10.6023/cjoc201610017
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 31370575).

To develop isopimaric acid derivatives with high bioactivity, fifteen acyl (amide) thiourea derivatives containing isopimaric acid skeleton were synthesized and confirmed by FT-IR, 1H NMR, 13C NMR and HRMS or elemental analysis. All the compounds were evaluated for their antibacterial and anticancer activity. Most of the compounds showed siginificant inhibitory activity which was higher than that of isopiamric acid against the Candida Albicans. At the concentration of 100 μmol/L, many compounds exhibited pronounced inhibitory effects on human melanoma cells (A375) and prostatic carcinoma (PC-3) cell lines, especially compounds N-isopimaric acyl-N'-(3-methylphenyl)sulfourea (3c) and N-isopimaric acylamino-N'-(4-fluorophenyl) sulfourea (6b) have the best anticancer activity, both with the inhibitory rate of over 90%.

Key words: isopimaric acid, acylthiourea, antibacterial activity, anticancer activity, structure-activity relationship