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  • Title: Discovery of novel selective inhibitors for EGFR-T790M/L858R.
    Author: Bai F, Liu H, Tong L, Zhou W, Liu L, Zhao Z, Liu X, Jiang H, Wang X, Xie H, Li H.
    Journal: Bioorg Med Chem Lett; 2012 Feb 01; 22(3):1365-70. PubMed ID: 22227214.
    Abstract:
    Through a receptor-based and ligand-based combined virtual screening protocol, 21 novel compounds covering 15 scaffolds were identified as novel inhibitors for EGFR-T790M/L858R, among which, 12 of them were identified as selective inhibitors for EGFR-T790M/L858R to wild-type EGFR, and 5 of them exhibited 'dual-effective' to wild-type and mutant EGFR. Meanwhile, their antiproliferative effects toward EGFR high-expressing human lung cancer cell (A549), epidermoid carcinoma cell (A431), and the mutant EGFR-dependent cell (NCI-H1975) were also evaluated.
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