Design, Synthesis and Biological Evaluation of Quinoxalin-2(1H)-one Derivatives as EGFR Tyrosine Kinase Inhibitors

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


Download PDF Flyer




Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

Design, Synthesis and Biological Evaluation of Quinoxalin-2(1H)-one Derivatives as EGFR Tyrosine Kinase Inhibitors



Anti-Cancer Agents in Medicinal Chemistry, 15(2): 267-273.

Author(s): Xuemei Qin, Xiao Han, Liming Hu, Zhipeng Li, Zhufeng Geng, Zhanyang Wang, Chengchu Zeng and Xiangqian Xiao.

Affiliation: College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China.

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 designin strategy.




Keywords:

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



Purchase Online Order Reprints Order Eprints Rights and Permissions




Article Details

Volume: 15
Issue Number: 2
First Page: 267
Last Page: 273
Page Count: 7
DOI: 10.2174/187152061502150116173357
Price: $58
Advertisement

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2016 Bentham Science