Synthesis and anti-proliferation activity of mogrol derivatives bearing quinoline and triazole moieties

被引：12

作者：

Song, Jing-Ru ^{[1
]}

Li, Na ^{[1
]}

Li, Dian-Peng ^{[1
]}

机构：

[1] Chinese Acad Sci, Guangxi Inst Bot, Guangxi Key Lab Funct Phytochem Res & Utilizat, Guilin 541006, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2021年 / 42卷

关键词：

Mogrol; Structural modification; Quinoline; Triazole; Lung cancer; HYBRIDS; DESIGN;

D O I：

10.1016/j.bmcl.2021.128090

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel derivatives based on mogrol were designed and synthesized in attempt to improve anti-lung cancer activity. The cytotoxicity against human lung cancer cells including A549 and NCI-H460 were performed by Cell Counting Kit-8 (CCK8) assay in vitro. The screening result showed that compound 8f exhibited the strongest activity with an IC50 value of 4.47 mu M against A549 cell, and could induce the cell apoptosis in a dosedependent manner and arrest cell cycle at G0/G1 phase. Besides, compound 8f displayed anti-proliferation effect on A549 cell through inhibiting phosphorylation of signal transducer and activator of transcription 3 (STAT3). Furthermore, compared with morgol, compound 10a significantly improved the cytotoxicity against NCI-H460 with the IC50 value of 17.13 mu M. The research stimulated the development of potential therapeutic agent for lung cancer from the natural mogrol.

引用

页数：5

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