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Design, synthesis and biological evaluation of tryptamine salicylic acid derivatives as potential antitumor agents.

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成果类型:
期刊论文
作者:
Xiong, Runde;He, Dongxiu;Deng, Xiangping;Liu, Juan;Lei, Xiaoyong;...
通讯作者:
Tang, Guotao
作者机构:
[Deng, Xiangping; Xie, Zhizhong; Liu, Juan; Lei, Xiaoyong; Tang, Guotao; He, Dongxiu; Peng, Junmei; 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] Jiuzhitang Co Ltd, Changsha, Hunan, Peoples R China.
通讯机构:
[Tang, Guotao] 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:
2 hydroxy 3 methyl n [2 (5 methyl 1h indol 3 yl)ethyl] benzamide;2 hydroxy 4 methyl n [2 (5 methyl 1h indol 3 yl)ethyl] benzamide;2 hydroxy n [2 (1h indol 3 yl)ethyl] 3 methyl benzamide;2 hydroxy n [2 (1h indol 3 yl)ethyl] 4 methyl benzamide;2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl]benzamide;4 chloro 2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;4 chloro 2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl]benzamide;4 chloro n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxybenzamide;5 bromo 2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;5 bromo 2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl] benzamide;5 bromo n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxybenzamide;5 bromo n [2 (5 chloro 1h indol 3 yl) ethyl] 2 hydroxybenzamide;5 chloro 2 hydroxy n [2 (1h indol 3 yl)ethyl]benzamide;5 chloro 2 hydroxy n [2 (5 methyl 1h indol 3 yl)ethyl]benzamide;5 chloro n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxybenzamide;antineoplastic agent;hexokinase;hexokinase 2;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy 3 methyl benzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy 3 methylbenzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy 4 methylbenzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 2 hydroxy benzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 4 chloro 2 hydroxybenzamide;n [2 (5 bromo 1h indol 3 yl)ethyl] 5 chloro 2 hydroxybenzamide;n [2 (5 chloro 1h indol 3 yl) ethyl] 2 hydroxy 4 methylbenzamide;n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxy 3 methylbenzamide;n [2 (5 chloro 1h indol 3 yl)ethyl] 2 hydroxy benzamide;salicylic acid derivative;unclassified drug;A-549 cell line;antineoplastic activity;antiproliferative activity;apoptosis;Article;cancer inhibition;cell migration;concentration response;down regulation;drug design;drug determination;drug potency;drug structure;drug synthesis;drug targeting;flow cytometry;G2 phase cell cycle checkpoint;HeLa cell line;Hep-G2 cell line;in vitro study;MCF-7 cell line;priority journal;protein expression;structure activity relation;Western blotting
期刊:
RSC Medicinal Chemistry
ISSN:
2632-8682
年:
2019
卷:
10
期:
4
页码:
573-583
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), Innovation Platform Open Foundation of the Education, Department of Hunan province (contract grant number 16K079, 17K082) and Graduate Student Science Foundation of the University of South China (2018490).
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 tryptamine salicylic acid derivatives were synthesized and their antiproliferative activity against MGC-803, MCF-7, HepG2, A549 and HeLa cell lines was evaluated. The structure-activity relationship (SAR) study revealed that different substitutions of the C5 and C3′-C5′ positions have certain effects on the anti-proliferation activity. The growth assay revealed that N-[2-(5-bromo-1H-indol-3-yl)-ethyl]-2-hydroxy-3-methyl-benzamide (E20) showed the most potent and broad-spectrum anticancer inhibition of all the cell lines evaluated,...

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