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作者:

Qin, Xuemei (Qin, Xuemei.) | Han, Xiao (Han, Xiao.) | Hu, Liming (Hu, Liming.) (学者:胡利明) | Li, Zhipeng (Li, Zhipeng.) | Geng, Zhufeng (Geng, Zhufeng.) | Wang, Zhanyang (Wang, Zhanyang.) | Zeng, Chengchu (Zeng, Chengchu.) (学者:曾程初) | Xiao, Xiangqian (Xiao, Xiangqian.)

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Scopus SCIE PubMed

摘要:

With the successful use of gefitinib and erlotinib in clinic, some potent EGFR tyrosine kinase receptor inhibitors have gained widespread concern in the treatment of ovarian or non-small-cell lung cancer. However, the emergence of EGFR-activating mutations resist to the drugs, there is an impending need to design new inhibitor targeted EGFR. Furthermore, the understanding of mutual effect between EGFR and drug has been available, it has become a hot spot for the research of anticancer drugs. We have designed and synthesized a series of 6-methoxy-7-(3-morpholinopropoxy)-1-(2-phenoxyethyl)-quinoxalin-2(1H)-one derivatives as novel EGFR inhibitors. Most of the compounds have showed inhibitory activity toward EGFR kinase. This work has demonstrated it is possible to construct a new type of EGFR protein kinase inhibitor using a design-in strategy.

关键词:

Anticancer EGFR inhibitor kinase assay molecular docking quinazolin-2(1H)-one tyrosine kinase

作者机构:

  • [ 1 ] [Qin, Xuemei]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 2 ] [Han, Xiao]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 3 ] [Hu, Liming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 4 ] [Li, Zhipeng]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 5 ] [Wang, Zhanyang]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 6 ] [Zeng, Chengchu]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 7 ] [Xiao, Xiangqian]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China
  • [ 8 ] [Geng, Zhufeng]Beijing Normal Univ, Analyt & Testing Ctr, Beijing 100875, Peoples R China

通讯作者信息:

  • 胡利明

    [Hu, Liming]Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

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来源 :

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY

ISSN: 1871-5206

年份: 2015

期: 2

卷: 15

页码: 267-273

2 . 8 0 0

JCR@2022

ESI学科: PHARMACOLOGY & TOXICOLOGY;

ESI高被引阀值:122

JCR分区:2

中科院分区:3

被引次数:

WoS核心集被引频次: 7

SCOPUS被引频次: 7

ESI高被引论文在榜: 0 展开所有

万方被引频次:

中文被引频次:

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