Discovery of novel selective inhibitors for EGFR-T790M/L858R.

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Bai F, Liu H, Tong L, Zhou W, Liu L, Zhao Z, Liu X, Jiang H, Wang X, Xie H, Li H

Discovery of novel selective inhibitors for EGFR-T790M/L858R.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1365-70. doi: 10.1016/j.bmcl.2011.12.067. Epub 2011 Dec 17.

PubMed ID

22227214 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Lapatinib	Epidermal growth factor receptor	IC 50 (nM)	8	N/A	N/A	Details