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  • Title: Synthesis and in vitro biological evaluation of novel quinazoline derivatives.
    Author: Zhang Y, Zhang Y, Liu J, Chen L, Zhao L, Li B, Wang W.
    Journal: Bioorg Med Chem Lett; 2017 Apr 01; 27(7):1584-1587. PubMed ID: 28238614.
    Abstract:
    A series of novel 4-arylamino-6-(5-substituted furan-2-yl)quinazoline derivatives were designed, synthesized and evaluated on biological activities in vitro. Compound 2a, 3a and 3c exhibited highly anti-proliferation activities on all tested tumor cell lines including SW480, A549, A431 and NCI-H1975 cells. Especially, compound 2a not only exhibited strong anti-proliferation activities against the tumor cell lines which expressed wild type or mutant EGFRL858R/T790M, but also showed the most potent inhibitory activity toward wild type EGFR (IC50=5.06nM). The result of docking with EGFR suggested the binding mode of 2a was similar to that of lapatinib. While Western-blot analyses showed 2a obviously inhibited the activation of EGFR, Akt and Erk1/2 in lung cancer cells at indicated concentration. It is believed that this work would be very useful for developing a new series of TKIs targeting EGFR.
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