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熊果酸衍生物的合成及抗肿瘤活性的研究

孟艳秋 李思竹

药学研究2016,Vol.35Issue(9):514-516,3.
药学研究2016,Vol.35Issue(9):514-516,3.DOI:10.13506/j.cnki.jpr.2016.09.005

熊果酸衍生物的合成及抗肿瘤活性的研究

Synthesis and anti-tumor activity of ursolic acid derivatives

孟艳秋 1李思竹1

作者信息

  • 1. 沈阳化工大学制药工程教研室,辽宁 沈阳 110142
  • 折叠

摘要

Abstract

Objective To study the inhibitory ability of pentacyclic triterpenoids novel compounds to cancer cells,and thus find new anticancer drugs.Methods Structure of natural product-ursolic acid was modified for increasing its antitumor activity.Eight new derivatives of ursolic acid were designed and synthesized by the structure modified at C-2 hydrogen,C-3 hydroxyl group,C-28 carboxy group and ring A. Results The antitumor activities of target compounds were evaluated by MTT assay.The results indicated that all the compounds had a degree of inhibition on cell proliferation of HeLa,HepG2 and BGC-823 cells.Compound I3 showed strong inhibitory activity to HeLa,HepG2 and BGC-823 cells.Conclusion The com-pounds showed strong inhibitory activity on these three kinds of tumor cells,significantly higher than the listed drug Ge-fitinib,and were worth to be intensively studied further.

关键词

熊果酸衍生物/抗肿瘤活性/抑制剂

Key words

Ursolic acid derivatives/Antitumor activity/Inhibitor

分类

医药卫生

引用本文复制引用

孟艳秋,李思竹..熊果酸衍生物的合成及抗肿瘤活性的研究[J].药学研究,2016,35(9):514-516,3.

药学研究

2095-5375

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