Discovery of novel selective inhibitors for EGFR-T790M/L858R.
Article Details
- CitationCopy to clipboard
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]
- 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