Design, synthesis, and preliminary biological evaluation of 3′,4′,5′-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents

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成果类型：

期刊论文

作者：

Deng, Xiangping;Liu, Renbo;Li, Junjian;Li, Zhongli;Liu, Juan;...

通讯作者：

Tang, Guotao

作者机构：

[Deng, Xiangping; Xie, Zhizhong; Li, Zhongli; Liu, Renbo; Liu, Juan; Lei, Xiaoyong; Tang, Guotao; Li, Junjian; Xiong, Runde; Zheng, Xing] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.

通讯机构：

[Tang, Guotao] U

Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.

语种：

英文

关键词：

4 [5 (4 methyl 1 piperazinyl)[2,5' bi 1h benzimidazol] 2' yl]phenol;6 phosphofructokinase;7 hydroxy 2 (3,4,5 trimetocyphenyl) 4h chromen 4 one;antineoplastic agent;flavonoid;fluorouracil;hypoxia inducible factor 1alpha;salicylic acid derivative;tubulin;unclassified drug;antineoplastic activity;apoptosis;Article;cell cycle;colony formation;controlled study;crystal structure;drug cytotoxicity;drug design;drug synthesis;female;flow cytometry;HCT 116 cell line;human;human cell;priority journal;Western blotting

期刊：

NEW JOURNAL OF CHEMISTRY

ISSN：

1144-0546

年：

2019

卷：

期：

页码：

1874-1884

DOI：

10.1039/c8nj04533j

基金类别：

This work was financially supported by Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study (0223-0002-0002000-49) and Innovation Platform Open Foundation of Education, Department of Hunan province (contract grant number 16K079, 17K082).

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：

According to the pharmacophore combination principle, a set of new 3′,4′,5′-trimethoxy flavonoid salicylate derivatives were designed, synthesized, and evaluated for biological activity. The cytotoxicity evaluation revealed that compound 10v exhibited higher potency than 5-Fu against HCT-116 cells. Preliminary biological activity studies showed that compound 10v could inhibit the colony formation and migration of HCT-116 cells. Besides, the Hoechst 33258 staining assay and flow cytometry revealed that treatment with compound 10v induced the ...

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Design, synthesis, and preliminary biological evaluation of 3′,4′,5′-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents

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