Rational Synthesis and Preliminary Anti-cancer Activities of 18β-Glycyrrhetinic Acid Derivatives Containing Pyridinecarboxamide

doi:10.6023/cjoc201410013

Chin. J. Org. Chem. ›› 2015, Vol. 35 ›› Issue (4): 835-842.DOI: 10.6023/cjoc201410013 Previous Articles Next Articles

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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

陈凑喜^a,b, 魏梦雪^a,b, 李学强^a,b, 李天才^a,b, 周学章^c

a 宁夏大学化学化工学院银川 750021;
b 宁夏大学宁夏天然药物工程技术研究中心银川 750021;
c 宁夏大学西部特色生物资源保护与利用教育部重点实验室银川 750021

收稿日期:2014-10-09 修回日期:2014-12-07 发布日期:2014-12-23
通讯作者: 李学强 E-mail:lixq@nxu.edu.cn
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

Chen Couxi^a,b, Wei Mengxue^a,b, Li Xueqiang^a,b, Li Tiancai^a,b, Zhou Xuezhang^c

a School of Chemistry and Chemical Engineering, Ningxia University, Yinchuan 750021;
b Ningxia Development Center of Natural Products and Medication, Yinchuan 750021;
c Key Laboratory of Ministry of Education for Protection and Utilization of Special Biological Resources in Western China, Ningxia University, Yinchuan 750021

Received:2014-10-09 Revised:2014-12-07 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).

1. Rational Synthesis and Preliminary Anti-cancer Activities of 18β-Glycyrrhetinic Acid Derivatives Containing Pyridinecarboxamide.PDF(42309KB)

Abstract

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

Cite this article

Chen Couxi, Wei Mengxue, Li Xueqiang, Li Tiancai, Zhou Xuezhang. Rational Synthesis and Preliminary Anti-cancer Activities of 18β-Glycyrrhetinic Acid Derivatives Containing Pyridinecarboxamide[J]. Chin. J. Org. Chem., 2015, 35(4): 835-842.

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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

Rational Synthesis and Preliminary Anti-cancer Activities of 18β-Glycyrrhetinic Acid Derivatives Containing Pyridinecarboxamide

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