Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 2, Pages 638-643Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.12.036
Keywords
EGFR; Kinase inhibitor; T790M; Mutant selective
Categories
Funding
- NCI NIH HHS [R01 CA130876-03, R01 CA130876, R01 CA135257, R01 CA130876-02, R01 CA130876-01A1, R01 CA130876-04, P01 CA154303] Funding Source: Medline
- NIGMS NIH HHS [P41 GM079575-01, P41 GM079575-02, P41 GM079575, P41 GM079575-03, P41 GM079575-03S1] Funding Source: Medline
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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