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Article

Modification of osimertinib to discover new potent EGFRC797S-TK inhibitors.

European journal of medicinal chemistry - 5 Dec 2023

Xi Xiao-Xiao, Zhao Hong-Yi, Mao Yu-Ze, Xin Minhang, Zhang San-Qi

Abstract excerpt

The EGFRC797S mutation is a dominant mechanism of acquired resistance after the treatment of non-small cell lung cancer (NSCLC) with osimertinib in clinic. To date, there is no inhibitor approved to overcome the resistance caused by osimertinib. In this study, a series of compounds with phenylamino-pyrimidine scaffold deriving from osimertinib were designed, synthesized and evaluated as fourth-generation...

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Identifiers

PMID: 37839342
DOI: 10.1016/j.ejmech.2023.115865

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