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
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)