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Synthesis and biological evaluation of novel 5,6,7-trimethoxy flavonoid salicylate derivatives as potential anti-tumor agents

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成果类型:
期刊论文
作者:
Liu, Renbo;Deng, Xiangping;Peng, Yijiao;Feng, Wanshi;Xiong, Runde;...
通讯作者:
Tang, Guotao
作者机构:
[Deng, Xiangping; Xie, Zhizhong; Liu, Renbo; Lei, Xiaoyong; Peng, Yijiao; Zou, Yang; Tang, Guotao; Feng, Wanshi; Xiong, Runde; Zheng, Xing] Univ South China, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Inst Pharm & Pharmacol, Hengyang City, Peoples R China.
[Deng, Xiangping; Liu, Renbo; Tang, Guotao] Hunan Prov Key Lab Tumor Microenvironm Respons Dr, Hengyang City, Hunan, Peoples R China.
[Tang, Guotao] Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
通讯机构:
[Tang, Guotao] U
Univ South China, Inst Pharm & Pharmacol, Hengyang 421001, Hunan, Peoples R China.
语种:
英文
关键词:
Anti-tumor;Flavonoid;Glycolysis;HIF-1alpha;Microtubules
期刊:
Bioorganic Chemistry
ISSN:
0045-2068
年:
2020
卷:
96
页码:
103652
基金类别:
This work was financially supported by Hunan Provincial Key Laboratory of Tumor Microenvironment Responsive Drug Research (Approval number: 2019-56) and Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study.
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:
5,6,7-Trimethoxy flavonoid salicylate derivatives were designed by the joining of three important pharmacophores (TMP, flavonoid, and SA) according to the combination principle. A series of novel trimethoxy flavonoid salicylate derivatives were synthesized and their in vitro anti-tumor activities were evaluated. Among these derivatives, compound 7f exhibited excellent antiproliferative activity against HGC-27 cells and MGC-803 cells with IC50 values of 10.26 ± 6.94 μM and 17.17 ± 3.03 μM, respectively. Subsequently, the effects on cell colo...

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