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

doi:10.6023/cjoc201805011

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

Notes

新型黄酮-Tröger's碱类衍生物的合成及其生物活性

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

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 E-mail:wuhui72@jsnu.edu.cn
基金资助:
江苏省高校优势学科建设工程项目、江苏省高校自然科学研究重点项目（No.15KJA180002）和江苏师范大学博士学位教师科研支持项目（No.17XLR023）资助项目.

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

Yuan Rui^a, Wang Yuanjiang^b, Huang Shuying^b, Dou Pengfei^b, Zhang Longyan^b, Chen Wen^b, Ren Xuanxuan^b, Zhou Shengliang^a, Wan Yu^a, Wu Hui^a,b

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 E-mail:wuhui72@jsnu.edu.cn
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).

1. Synthesis and Biological Evaluation of Novel Flavonoid-Substituted Tröger's Bases.PDF(746KB)

Abstract

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

Cite this article

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]. Chin. J. Org. Chem., 2018, 38(12): 3338-3344.

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新型黄酮-Tröger's碱类衍生物的合成及其生物活性

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

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