Design and synthesis of 4(1H)-quinolone derivatives as autophagy inducing agents by targeting ATG5 protein

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成果类型：

期刊论文

作者：

Jia, Yifan;Yu, Difei;Huang, Qiuhua;Zhang, Xiaodong;Qiu, Liqin;...

通讯作者：

Liu, Wenbin;Du, Runlei;Cao, Rihui

作者机构：

[Jia, Yifan] Wuhan Univ, Dept Pain Management, Renmin Hosp, Wuhan 430060, Peoples R China.

[Liu, Wenbin] Wuhan Polytech Univ, Coll Hlth Sci & Nursing, Wuhan 430023, Peoples R China.

[Zhang, Xiaodong; Yu, Difei; Du, Runlei] Wuhan Univ, Coll Life Sci, Hubei Key Lab Cell Homeostasis, Wuhan 430072, Peoples R China.

[Huang, Qiuhua; Cao, Rihui; Qiu, Liqin] Sun Yat Sen Univ, Sch Chem, Guangzhou 510275, Peoples R China.

通讯机构：

[Liu, Wenbin; Du, Runlei] W

[Cao, Rihui] S

Wuhan Polytech Univ, Coll Hlth Sci & Nursing, Wuhan 430023, Peoples R China.

Wuhan Univ, Coll Life Sci, Hubei Key Lab Cell Homeostasis, Wuhan 430072, Peoples R China.

Sun Yat Sen Univ, Sch Chem, Guangzhou 510275, Peoples R China.

语种：

英文

关键词：

7 chloro 4(1h) quinolone derivative;antineoplastic agent;autophagy related protein 5;quinolone derivative;unclassified drug;antiproliferative activity;Article;autophagy (cellular);colorectal cancer cell line;drug design;drug mechanism;drug synthesis;drug targeting;human;human cell;MTT assay;priority journal;tumor cell line

期刊：

LETTERS IN DRUG DESIGN & DISCOVERY

ISSN：

1570-1808

年：

2020

卷：

期：

页码：

884-890

DOI：

10.2174/1570180816666191122113045

基金类别：

This work was supported by grants from the Natural Science Foundation of Guangdong Province [S2013010012138 and 2016A030313349] and the National Natural Science Foundation of China grant [81872271, 31501148, and 81402994].

机构署名：

本校为通讯机构

院系归属：

医学与健康学院

摘要：

Background: Quinolines have been characterized as a class of potential antitumor agents, and a large number of natural and synthetic quinolines acting as antitumor agents were reported. Methods: A series of 7-chloro-4(1H)-quinolone derivatives were synthesized. The antiproliferative effect of these compounds was evaluated by MTT assay against five human tumor cell lines. The mechanism of action of the selected compound 7h was also investigated. Results and Discussion: Most of the compounds had more potent antiproliferative activities than the l...

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Design and synthesis of 4(1H)-quinolone derivatives as autophagy inducing agents by targeting ATG5 protein

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