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.
Fang Bai  1 ,  Hongyan Liu ,  Linjiang Tong ,  Wei Zhou ,  Li Liu ,  Zhenjiang Zhao ,  Xiaofeng Liu ,  Hualiang Jiang ,  Xicheng Wang ,  Hua Xie ,  Honglin Li
Affiliations
  • 1. Faculty of Chemical, Environmental and Biological Science and Technology, Dalian University of Technology, Dalian 116023, China.
PMID: 22227214 DOI: 10.1016/j.bmcl.2011.12.067
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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