Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors

[Image: see text] Allosteric kinase inhibitors represent a promising new therapeutic strategy for targeting kinases harboring oncogenic driver mutations in cancers. Here, we report the discovery, optimization, and structural characterization of allosteric mutant-selective EGFR inhibitors comprising...

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Bibliographic Details
Published in:ACS Med Chem Lett
Main Authors: De Clercq, Dries J. H., Heppner, David E., To, Ciric, Jang, Jaebong, Park, Eunyoung, Yun, Cai-Hong, Mushajiang, Mierzhati, Shin, Bo Hee, Gero, Thomas W., Scott, David A., Jänne, Pasi A., Eck, Michael J., Gray, Nathanael S.
Format: Artigo
Language:Inglês
Published: American Chemical Society 2019
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC6862338/
https://ncbi.nlm.nih.gov/pubmed/31749909
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00381
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