Discovery of selective irreversible inhibitors for EGFR-T790M.

Basic Information

ID: ALA1641501

Journal: Bioorg Med Chem Lett

Title: Discovery of selective irreversible inhibitors for EGFR-T790M.

Authors: Zhou W, Ercan D, Jänne PA, Gray NS.

Abstract: Targeting the epidermal growth factor receptor kinase (EGFR) with ATP-competitive kinase inhibitors results in dramatic but short-lived responses in patients with EGFR mutant non small cell lung cancer. A series of novel covalent EGFR kinase inhibitors with selectivity for the clinically relevant T790M 'gatekeeper' resistance mutation relative to wild-type EGFR were discovered by library screening. A representative compound 3i was obtained through a systematic SAR study guided by mutant EGFR-dependent cellular proliferation assays.

CiteXplore: 21208802

DOI: 10.1016/j.bmcl.2010.12.036

Patent ID: ┄