Article
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Bioorganic & medicinal chemistry letters - 15 Jan 2023
Huang Wei-Sheng, Li Feng, Gong Yongjin, Zhang Yun, Youngsaye Willmen, Xu Yongjin, Zhu Xiaotian, Greenfield Matthew T, Kohlmann Anna, Taslimi Paul M, Toms Angela, Zech Stephan G, Zhou Tianjun, Das Biplab, Jang Hyun G, Tugnait Meera, Ye Yihua E, Gonzalvez Francois, Baker Theresa E, Nadworny Sara, Ning Yaoyu, Wardwell Scott D, Zhang Sen, Gould Alexandra E, Hu Yongbo, Lane Weston, Skene Robert J, Zou Hua, Clackson Tim, Narasimhan Narayana I, Rivera Victor M, Dalgarno David C, Shakespeare William C
Abstract excerpt
In the treatment of non-small cell lung cancer (NSCLC), patients harboring exon 20 insertion mutations in the epidermal growth factor receptor (EGFR) gene (EGFR) have few effective therapies because this subset of mutants is generally resistant to most currently approved EGFR inhibitors. This report describes the structure-guided design of a novel series of potent, irreversible inhibitors of EGFR exon 20...
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