Article
Design, synthesis and biological evaluation of potent EGFR kinase inhibitors against 19D/T790M/C797S mutation.
Bioorganic & medicinal chemistry letters - 15 Aug 2020
Su Zhicheng, Yang Tingyuan, Wang Jie, Lai Mengzhen, Tong Linjiang, Wumaier Gulinuer, Chen Zhuo, Li Shengqing, Li Honglin, Xie Hua, Zhao Zhenjiang
Abstract excerpt
The efficacy of EGFR inhibitors is frequently affected by acquired resistance. EGFR19D/T790M/C797S mutation is one of the primary reasons for the emergence of resistance after treatment with the third-generation EGFR inhibitors such as AZD9291, CO1686 and Olmutinib. To overcome the resistance mutation 19D/T790M/C797S, we designed and prepared a series of indole derivatives with the terminal hydroxyl of alkyl...
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