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Synthesis and evaluation of antitumour activity in vitro and in vivo of chrysin salicylate derivatives

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成果类型:
期刊论文
作者:
Deng, Xiangping;Zhao, Zihao;Xiong, Shujuan;Xiong, Runde;Liu, Juan;...
通讯作者:
Liu, Yunmei;Tang, Guotao
作者机构:
[Wang, Zhe; Liu, Yunmei; Zou, Liu; Liu, Juan; Tang, Guotao; Zheng, Xing; Deng, Xiangping; Xie, Zhizhong; Liu, YM; Tang, GT; Lei, Xiaoyong; Xiong, Shujuan; Zhao, Zihao; Xiong, Runde; Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.
[Zhao, Zihao] Xiangtan Cent Hosp, Pharm Dept, Xiangtan, Peoples R China.
[Chen, Yanming] Mu Dan Jiang You Bo Pharmacert Co Ltd, Mudanjiang, Peoples R China.
通讯机构:
[Liu, YM; Tang, GT] U
Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.
语种:
英文
关键词:
antineoplastic agent;chrysin;chrysin salicylate derivative;fluorouracil;salicylic acid derivative;unclassified drug;antineoplastic agent;chrysin;flavonoid;salicylic acid derivative;animal experiment;animal model;animal tissue;antineoplastic activity;Article;cancer cell line;cell cycle G1 phase;cell cycle S phase;controlled study;drug efficacy;drug megadose;drug potency;drug screening;drug structure;drug synthesis;flow cytometry;Hep-G2 cell line;human;human cell;IC50;in vitro study;in vivo study;MCF-7 cell line;MFC cell line;MGC-803 cell line;mouse;nonhuman;stomach carcinoma;animal;cell proliferation;drug effect;structure activity relation;synthesis;tumor cell line;Animals;Antineoplastic Agents;Cell Line, Tumor;Cell Proliferation;Drug Screening Assays, Antitumor;Flavonoids;Hep G2 Cells;Humans;MCF-7 Cells;Mice;Salicylates;Structure-Activity Relationship
期刊:
Natural Product Research
ISSN:
1478-6419
年:
2018
卷:
32
期:
18
页码:
2178-2186
基金类别:
This work was supported in part by the Construct Program of the key Discipline in Hunan Province and Hunan Province Cooperative Innovation Center for Molecular Target New Drug study. The author thanks the Department of Laboratory Animal Science for the support of animals experiments.
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:
A series of chrysin salicylate derivatives as potential antitumour agents were synthesised and evaluated their antitumour activities in vitro and in vivo. Most of the compounds exhibited moderate to good activities against MCF-7 cells, HepG2 cells, MGC-803cells and MFC cells. Among them, compound 3f showed the most potent activity against MGC-803 cells and MFC cells with IC50 values of 23.83±3.68 and 27.34±5.21μM, respectively. The flow cytometry assay reconfirmed that compound 3f promoted the occurrence of tumour cells’ G1/S block under th...

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