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Author:

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

Indexed by:

Scopus SCIE PubMed

Abstract:

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.

Keyword:

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

Author Community:

  • [ 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

Reprint Author's Address:

  • 胡利明

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

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Source :

ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY

ISSN: 1871-5206

Year: 2015

Issue: 2

Volume: 15

Page: 267-273

2 . 8 0 0

JCR@2022

ESI Discipline: PHARMACOLOGY & TOXICOLOGY;

ESI HC Threshold:182

JCR Journal Grade:2

CAS Journal Grade:3

Cited Count:

WoS CC Cited Count: 8

SCOPUS Cited Count: 7

ESI Highly Cited Papers on the List: 0 Unfold All

WanFang Cited Count:

Chinese Cited Count:

30 Days PV: 13

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