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2014 , Vol. 34 >Issue 3: 600 - 604

DOI: https://doi.org/10.6023/cjoc201309034

研究简报

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
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  • 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

  网络出版日期: 2013-11-05

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.

收起

Synthesis and Biological Evaluation of 4-Dimethylamino Flavonoid Derivatives

  • Su Yabin ,
  • Hong Chen ,
  • Li Qian ,
  • Luo Wen ,
  • Wang Chaojie
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  • Key Laboratory of Natural Medicine and Immuno-Engineering of Henan Province, Henan University, Kaifeng 475004

Received date: 2013-09-26

  Revised date: 2013-10-29

  Online 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).

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摘要

设计合成了10个4-二甲氨基黄酮衍生物，产物结构均经1H NMR，ESI-MS和元素分析确认. 采用噻唑蓝（MTT）法测试了化合物对HepG2（人肝癌细胞）的抑制作用，结果表明目标化合物在30 mmol/L浓度下对HepG2细胞损伤均有一定的抑制作用，大部分化合物优于对照药物槲皮素，其中化合物5c，5e，5f和5j活性最强，抑制率分别为91.0%，90.1%，95.7%和92.1%，而且化合物5f在10 mmol/L浓度下对HepG2的抑制率为93.1%，具有深入研究的价值.

关键词： 黄酮; 衍生物; 合成; 抗肿瘤

本文引用格式

苏亚彬 , 洪琛 , 李骞 , 罗稳 , 王超杰 . 4-二甲氨基黄酮衍生物的合成及其活性评价[J]. 有机化学, 2014 , 34(3) : 600 -604 . DOI: 10.6023/cjoc201309034

Abstract

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

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