- Discovery of selective irreversible inhibitors for EGFR-T790M
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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.
- Zhou, Wenjun,Ercan, Dalia,Jaenne, Pasi A.,Gray, Nathanael S.
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p. 638 - 643
(2011/03/18)
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- EGFR INHIBITORS AND METHODS OF TREATING DISORDERS
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The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
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Page/Page column 125
(2010/11/18)
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