Citation: Yuan Rui, Wang Yuanjiang, Huang Shuying, Dou Pengfei, Zhang Longyan, Chen Wen, Ren Xuanxuan, Zhou Shengliang, Wan Yu, Wu Hui. Synthesis and Biological Evaluation of Novel Flavonoid-Substituted Tröger's Bases[J]. Chinese Journal of Organic Chemistry, ;2018, 38(12): 3338-3344. doi: 10.6023/cjoc201805011 shu

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

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

Corresponding author: Wu Hui, wuhui72@jsnu.edu.cn
Received Date: 3 May 2018
Revised Date: 27 July 2018
Available Online: 5 December 2018
Fund Project: 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)the Priority Academic Program Development of Jiangsu Higher Education Institutions, the Major Project of the Natural Science Research of University in Jiangsu Province 15KJA180002the Aid Project for PhD Faculties in Jiangsu Normal University 17XLR023

Figures(4)

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.
- Tröger's base,
- flavonoid,
- bioactivity
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沈阳化工大学材料科学与工程学院沈阳 110142