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

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成果类型:
期刊论文
作者:
Wang, Zhe;Deng, Xiangping;Xiong, Runde;Xiong, Shujuan;Liu, Juan;...
通讯作者:
Zheng, Xing;Tang, Guotao
作者机构:
[Wang, Zhe; Deng, Xiangping; Liu, Juan; Lei, Xiaoyong; Xiong, Shujuan; Zheng, Xing; Tang, Guotao; Xiong, Runde; Cao, Xuan] Univ South China, Inst Pharm & Pharmacol, Hunan Prov Cooperat Innovat Ctr Mol Target New Dr, Hengyang, Peoples R China.
[Chen, Yanming] Mu Dan Jiang You Bo Pharmaceut Co Ltd, Mudanjiang, Peoples R China.
通讯机构:
[Zheng, X; 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:
3',4',5' trimethoxy flavonoid benzimidazole derivative;7 (2 bromoethoxy) 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 (3 bromopropoxy) 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 (4 bromobutoxy) 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 hydroxy 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [2 chloro 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [2 methyl 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [2 [trifluoromethyl] 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [5 methoxy 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [5 methyl 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [5,6 dimethyl 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [2 [6 nitro 1h benz[d]imidazol 1 yl]ethoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 (2 chloro 1h benz[d]imidazol 1 yl)propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [2 chloro 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [2 methyl 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [2 [trifluoromethyl] 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [5 methoxy 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [5 methyl 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [5,6 dimethyl 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [3 [6 nitro 1h benz[d]imidazol 1 yl]propoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [2 chloro 1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [2 methyl 1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;7 [4 [5 nitro 1h benz[d]imidazol 1 yl]butoxy] 2 (3,4,5 trimethoxyphenyl) 4h chromen 4 one;antineoplastic agent;benzimidazole derivative;flavonoid;fluorouracil;unclassified drug;unindexed drug;animal cell;antineoplastic activity;antiproliferative activity;apoptosis;Article;controlled study;cytotoxicity assay;drug design;drug synthesis;flow cytometry;G1 phase cell cycle checkpoint;human;human cell;IC50;in vitro study;in vivo study;mouse;nonhuman;priority journal;tumor growth
期刊:
RSC Medicinal Chemistry
ISSN:
2632-8682
年:
2018
卷:
9
期:
2
页码:
305-315
基金类别:
This work was financially supported by the Construct Program of the Key Discipline in Hunan province 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:
A series of 3′,4′,5′-trimethoxy flavonoids with benzimidazole linked by different chain alkanes have been designed and synthesized. The potential activity of these compounds as anti-tumor agents was evaluated by cytotoxicity assay in MGC-803 (human gastric cancer), MCF-7 (human breast cancer), HepG-2 (human hepatoma) and MFC (mouse gastric cancer) tumor cell lines. Among them, compound 15 7-(3-(2-chloro-1H-benzo[d]imidazol-1-yl)propoxy)-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one displayed the most potent antiproliferative activity, with IC5...

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