Design, Synthesis and Biological Evaluation of Quinoxalin-2(1H)-one Derivatives as EGFR Tyrosine Kinase Inhibitors
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
Keywords: Anticancer, EGFR inhibitor, kinase assay, molecular docking, quinazolin-2(1H)-one, tyrosine kinase.
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