Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors

[Image: see text] In nonsmall cell lung cancer (NSCLC), the threonine(790)–methionine(790) (T790M) point mutation of EGFR kinase is one of the leading causes of acquired resistance to the first generation tyrosine kinase inhibitors (TKIs), such as gefitinib and erlotinib. Herein, we describe the opt...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Wurz, Ryan P., Pettus, Liping H., Ashton, Kate, Brown, James, Chen, Jian Jeffrey, Herberich, Brad, Hong, Fang-Tsao, Hu-Harrington, Essa, Nguyen, Tom, St. Jean, David J., Tadesse, Seifu, Bauer, David, Kubryk, Michele, Zhan, Jinghui, Cooke, Keegan, Mitchell, Petia, Andrews, Kristin L., Hsieh, Faye, Hickman, Dean, Kalyanaraman, Nataraj, Wu, Tian, Reid, Darren L., Lobenhofer, Edward K., Andrews, Dina A., Everds, Nancy, Guzman, Roberto, Parsons, Andrew T., Hedley, Simon J., Tedrow, Jason, Thiel, Oliver R., Potter, Matthew, Radinsky, Robert, Beltran, Pedro J., Tasker, Andrew S.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2015
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4569876/
https://ncbi.nlm.nih.gov/pubmed/26396685
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00193
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