18β-甘草次酸吡啶酰胺衍生物的定向合成及其初步抗癌活性研究
收稿日期: 2014-10-09
修回日期: 2014-12-07
网络出版日期: 2014-12-23
基金资助
国家自然科学基金(Nos. 21462032, 21062014)、宁夏高等学校科学技术研究(No. NGY.2013171)和宁夏大学人才引进科研启动基金(No. 80020241)资助项目.
Rational Synthesis and Preliminary Anti-cancer Activities of 18β-Glycyrrhetinic Acid Derivatives Containing Pyridinecarboxamide
Received date: 2014-10-09
Revised date: 2014-12-07
Online published: 2014-12-23
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 21462032, 21062014), the University of Science and Technology Research Project in Nignxia Province (No. NGY.2013171) and the Research Starting Funds for Imported Talents, Ningxia University (No. 80020241).
陈凑喜 , 魏梦雪 , 李学强 , 李天才 , 周学章 . 18β-甘草次酸吡啶酰胺衍生物的定向合成及其初步抗癌活性研究[J]. 有机化学, 2015 , 35(4) : 835 -842 . DOI: 10.6023/cjoc201410013
Five novel containing pyridinecarboxamide 18β-glycyrrhetinic acid derivatives have been designed and synthesized following the concept of ‘active structural splice’. In vitro studies demonstrated that all derivatives showed strong anti-cancer activities in thiazolylblue (MTT) assay towards Hela cell lines. They were founded to inhibit the Hela cell lines prolifration and induce apoptosis as the lowest IC50 values was only 0.02 μmol·L-1. Under the same conditions, these showed lower IC50 of cells growth than that of cytarabine. All findings supported further optimization efforts based on 18β-glycyrrhetinic acid as a lead compound to develop potential anti-cancer drug candidates.
Key words： 18β-glycyrrhetinic acid; pyridine; amide; derivative; anti-tumor activity
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