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3种香叶基取代黄烷酮的合成及抗肿瘤活性

马涛 杨金会 牛明杰 叶子平 李方辉

应用化学2017,Vol.34Issue(10):1140-1149,10.
应用化学2017,Vol.34Issue(10):1140-1149,10.DOI:10.11944/j.issn.1000-0518.2017.10.160494

3种香叶基取代黄烷酮的合成及抗肿瘤活性

Total Synthesis and Antitumor Activity of Three 6-Geranylated Flavanones

马涛 1杨金会 1牛明杰 1叶子平 1李方辉1

作者信息

  • 1. 宁夏大学化学化工学院 银川750021
  • 折叠

摘要

Abstract

Three geranylated flavanones isolated from the bark of Paulownia tomentosa were synthesized from phloroacetophenone and substituted hydroxybenzaldehydes via substitution,protection of phenolic hydroxyl group,aldol condensation,cyclization and deprotection reactions. Their structures were confirmed by proton and carbon(1 H and 13 C)nuclear magnetic resonance(NMR)and high resolution mass spectrometry(HRMS). The inhibition assay of these flavanones against A459 cell by methyl thiazolyl tetrazolium (MTT )protocol, indicates that compound 2 exihibits the highest activity with an half maximal inhibitory concentration (IC50 ) value at 25. 6 μmol/L. This study provides a suggestion for drug development based on geranylated flavanone scaffold.

关键词

毛泡桐/香叶基黄酮/黄烷酮/全合成/抗肿瘤活性

Key words

Paulownia tomentosa/geranylated flavanones/flavanone/total synthesis/antitumor activity

分类

化学化工

引用本文复制引用

马涛,杨金会,牛明杰,叶子平,李方辉..3种香叶基取代黄烷酮的合成及抗肿瘤活性[J].应用化学,2017,34(10):1140-1149,10.

基金项目

国家自然科学基金项目资助(21362025) Supported by the National Natural Science Foundation of China(No. 21362025) (21362025)

应用化学

OA北大核心CSCDCSTPCD

1000-0518

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