Design, synthesis, and biological evaluation of 3 \',4 \',5 \'-trimethoxy evodiamine derivatives as potential antitumor agents - 成果

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Design, synthesis, and biological evaluation of 3 ',4 ',5 '-trimethoxy evodiamine derivatives as potential antitumor agents

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作者信息关键词期刊信息基础信息归属信息摘要

成果类型：

期刊论文

作者：

Peng, Yijiao;Xiong, Runde;Li, Zhen;Peng, Junmei;Xie, Zhi-Zhong;...

通讯作者：

He, Dongxiu;Tang, Guotao

作者机构：

[Peng, Yijiao; Tang, Guotao; He, Dongxiu; Xiong, Runde] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang City, Peoples R China.

[Li, Zhen; Xie, Zhi-Zhong; Peng, Yijiao; Lei, Xiao-Yong; Tang, Guotao; He, Dongxiu; Peng, Junmei; Xiong, Runde] Hunan Prov Key Lab Tumor Microenvironm Respons Dr, Hengyang City, Hunan, Peoples R China.

[He, Dongxiu; Tang, Guotao] Univ South China, Hunan Prov Key Lab Tumour Microenvironm Respons D, 28 Chang Sheng Rd, Hengyang City 421001, Hunan, Peoples R China.

通讯机构：

[He, DX; Tang, GT] U

Univ South China, Hunan Prov Key Lab Tumour Microenvironm Respons D, 28 Chang Sheng Rd, Hengyang City 421001, Hunan, Peoples R China.

语种：

英文

关键词：

evodiamine;microtubule assembly;trimethoxy benzene

期刊：

Drug Development Research

ISSN：

0272-4391

年：

2021

卷：

期：

页码：

1021-1032

DOI：

10.1002/ddr.21806

基金类别：

Yijiao Peng and Runde Xiong contributed equally to this study. Hunan Postgraduate Research and Innovation Project, Grant/Award Number: CX20190751; Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, The natural science foundation of hunan province, Grant/Award Number: 2020JJ4534; Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research, Grant/Award Number: 2019-56

机构署名：

本校为第一且通讯机构

院系归属：

药学与生物科学学院

摘要：

AbstractA series of compounds bearing 3′,4′,5′‐trimethoxy module into the core structure of evodiamine were designed and synthesized. The synthesized compounds were screened in vitro for their antitumor potential. MTT results showed that compounds 14a–14c and 14i–14j had significant effects, with compound 14h being the most prominent, with an IC50 value of 3.3 ± 1.5μM, which was lower than evodiamine and 5‐Fu. Subsequent experiments further confirmed that compound 14h could inhibit cell proliferation and migration, and induce G2/M ph...

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Design, synthesis, and biological evaluation of 3 ',4 ',5 '-trimethoxy evodiamine derivatives as potential antitumor agents

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