Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (12): 3338-3344.DOI: 10.6023/cjoc201805011 Previous Articles     Next Articles



苑睿a, 王园江b, 黄树颖b, 窦鹏飞b, 张珑严b, 陈雯b, 任璇璇b, 周生亮a, 宛瑜a, 吴翚a,b   

  1. a 江苏师范大学江苏省药用植物生物技术重点实验室 徐州 221116;
    b 江苏师范大学化学化工学院 徐州 221116
  • 收稿日期:2018-05-03 修回日期:2018-07-27 发布日期:2018-09-05
  • 通讯作者: 吴翚
  • 基金资助:


Synthesis and Biological Evaluation of Novel Flavonoid-Substituted Tröger's Bases

Yuan Ruia, Wang Yuanjiangb, Huang Shuyingb, Dou Pengfeib, Zhang Longyanb, Chen Wenb, Ren Xuanxuanb, Zhou Shenglianga, Wan Yua, Wu Huia,b   

  1. a State Key Laboratory Cultivation Construction Base of Biotechnology on Med-edible Plant of Jiangsu Province, Jiangsu Normal University, Xuzhou, 221116;
    b School of Chemistry and Chemical Engineering, Jiangsu Normal University, Xuzhou 221116
  • Received:2018-05-03 Revised:2018-07-27 Published:2018-09-05
  • Contact: 10.6023/cjoc201805011
  • Supported by:

    Project supported by the Priority Academic Program Development of Jiangsu Higher Education Institutions, the Major Project of the Natural Science Research of University in Jiangsu Province (No. 15KJA180002) and the Aid Project for PhD Faculties in Jiangsu Normal University (No. 17XLR023).

A series of flavonoid-substituted Tröger's base analogues were synthesized via multi-step reaction. Their anti-cancer activities on the HepG2 hepatocellular carcinoma cell and antibacterial activities on four bacterial (Pseudomonas aeruginosa PAM1032, wild type Staphylococcus aureus, wild type Escherichia coli and Escherichia.coli-NMD-1) were evaluated. Two compounds were screened out because of their high inhibitory rate on Staphylococcus aureus at 1 μg/mL. The IC50 values of five products on the HepG2 (hepatocellular carcinoma cell) were lower than that of positive control paclitaxel (30.87 μg/mL), displaying their high inhibitory activity. The results indicated their potential applications in new drug development.

Key words: Tröger's base, flavonoid, bioactivity