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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Опубликовано в: :ACS Med Chem Lett
Главные авторы: 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.
Формат: Artigo
Язык:Inglês
Опубликовано: American Chemical Society 2015
Online-ссылка: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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