Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (3): 600-604.DOI: 10.6023/cjoc201309034 Previous Articles     Next Articles

Articles

4-二甲氨基黄酮衍生物的合成及其活性评价

苏亚彬, 洪琛, 李骞, 罗稳, 王超杰   

  1. 河南大学 天然药物与免疫工程重点实验室 开封 475004
  • 收稿日期:2013-09-26 修回日期:2013-10-29 发布日期:2013-11-05
  • 通讯作者: 罗稳,王超杰 E-mail:luowen83@hehu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos. 21172053,21302041);中国博士后基金(No. 2012M521391);河南省博士后基金(No. BH2011043)资助项目.

Synthesis and Biological Evaluation of 4-Dimethylamino Flavonoid Derivatives

Su Yabin, Hong Chen, Li Qian, Luo Wen, Wang Chaojie   

  1. Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University, Kaifeng 475004
  • Received:2013-09-26 Revised:2013-10-29 Published:2013-11-05
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21172053, 21302041), the Postdoctoral Science Foundation of China (No. 2012M521391) and the Postdoctoral Science Foundation of Henan Province (No. BH2011043).

Ten novel 4-dimethylamino flavonoid derivatives were designed and synthesized. The structures of these compounds were confirmed by 1H NMR, ESI-MS and elemental analysis. Their preliminary antitumor activity was evaluated by measuring their cytotoxic activity against the HepG2 cell line using thiazolyl blue tetrazolium bromide (MTT) assay. All ten compounds exhibited potent antitumor activity at 30 mmol/L. Some of the compounds displayed higher activity than the reference compound, quercetin. Compounds 5c, 5e, 5f and 5j were the most potent with inhibition rates of 91.0%, 90.1%, 95.7% and 92.1%, respectively. Moreover, compound 5f at 10 mmol/L showed an inhibition rate of 93.1%. Further investigation is needed.

Key words: flavonoid, derivative, synthesis, antitumor