title: Design, synthesis and biological evaluation of quinoxalin-2(1H)-one derivatives as EGFR tyrosine kinase inhibitors.
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.
authors.forename: Xuemei
authors.initials: X
authors.lastname: Qin
authors.forename: Xiao
authors.initials: X
authors.lastname: Han
authors.forename: Liming
authors.initials: L
authors.lastname: Hu
authors.forename: Zhipeng
authors.initials: Z
authors.lastname: Li
authors.forename: Zhufeng
authors.initials: Z
authors.lastname: Geng
authors.forename: Zhanyang
authors.initials: Z
authors.lastname: Wang
authors.forename: Chengchu
authors.initials: C
authors.lastname: Zeng
authors.affiliation: College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China. huliming@bjut.edu.cn.
authors.forename: Xiangqian
authors.initials: X
authors.lastname: Xiao
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D000069347:Erlotinib Hydrochloride; D000077156:Gefitinib; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011799:Quinazolines / Q000494:pharmacology; D011810:Quinoxalines / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D011810:Quinoxalines; D000069347:Erlotinib Hydrochloride; D066246:ErbB Receptors; D000077156:Gefitinib