版权说明 操作指南
首页 > 成果 > 详情

Design, synthesis and biological evaluation of flavonoid salicylate derivatives as potential anti-tumor agents

认领
导出
Link by DOI
反馈
分享
QQ微信 微博
成果类型:
期刊论文
作者:
Deng, Xiangping;Wang, Zhe;Liu, Juan;Xiong, Shujuan;Xiong, Runde;Cao, Xuan;Chen, Yanming;Zheng, Xing;Tang, Guotao
通讯作者:
Tang, G.
作者机构:
[Xiong, Shujuan; Deng, Xiangping; Xiong, Runde; Liu, Juan; Tang, Guotao; Cao, Xuan; Zheng, Xing; Wang, Zhe] Institute of Pharmacy and Pharmacology, Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study, University of South China, Hengyang, Hunan, 421001, China
[Chen, Yanming] Mudanjiang Youbo Pharmaceutical Co. Ltd, Mudanjiang, China
通讯机构:
[Tang, Guotao] 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:
Anti-proliferative activities - Anti-tumor activities - Anti-tumor agents - Biological evaluation - Breast carcinoma cells - Dose-dependent manner - Human tumor cells - Induced apoptosis
期刊:
RSC Advances
ISSN:
2046-2069
年:
2017
卷:
7
期:
61
页码:
38171-38178
基金类别:
Construct Program of the Key Discipline in Hunan Province; Hunan Province Cooperative Innovation Center for Molecular Target New Drug [Hunan Provincial Education Department document] [2014-405]; Department of Laboratory Animal Science
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 flavonoid salicylate derivatives containing trimethoxybenzene and a series of chrysin salicylate derivatives were synthesized for use as anti-tumor agents, and evaluated for antiproliferative activity using three human tumor cells: MCF-7 (breast carcinoma cells), HepG2 (liver carcinoma cells), MGC-803 (gastric carcinoma cells) and the mice tumor cells MFC (forestomach carcinoma cells). A substituent group of a suitable size and the trimethoxybenzene had a certain influence on the bioactivity of the flavonoid salicylate derivatives. Compound 2 and its salicylate derivatives 7a-7g containing the trimethoxybenzene exhibited more antiproliferative activity. Among them, compound 7g displayed the most potent antiproliferative activity against MGC-803 cells and MFC cells with the concentration causing 50% inhibition of cell growth (IC<inf>50</inf>) values of 11.05 &plusmn;1.58 &mu;M and 13.73 &plusmn;2.04 &mu;M, respectively. The flow cytometry results showed that compound 7g caused the cell cycle to be arrested in the G0/G1 phase and induced apoptosis of MFC cells in a dose-dependent manner. Furthermore, compound 7g showed good anti-tumor activity in vivo. These results suggested that compound 7g could be a new, potent anti-tumor candidate which should be optimized and evaluated further. &copy;2017 The Royal Society of Chemistry.

反馈

验证码:
看不清楚,换一个
确定
取消

成果认领

标题:
用户 作者 通讯作者
请选择
请选择
确定
取消

提示

该栏目需要登录且有访问权限才可以访问

如果您有访问权限,请直接 登录访问

如果您没有访问权限,请联系管理员申请开通

管理员联系邮箱:yun@hnwdkj.com