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Article

Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance.

Journal of medicinal chemistry - 9 Nov 2023

Zhu Yasheng, Ye Xiuquan, Shen Hao, Li Jiaxing, Cai Zeyu, Min Wenjian, Hou Yi, Dong Haojie, Wu Yuxing, Wang Liping, Wang Xiao, Xiao Yibei, Yang Peng

Abstract excerpt

Epidermal growth factor receptor (EGFR)-activating mutation is an important oncogenic driver of nonsmall cell lung cancer (NSCLC) patients. Osimertinib has been the first-line treatment for EGFR-mutated NSCLC. However, the tertiary C797S mutation leads to Osimertinib resistance by blocking the covalent binding of Cys797 to Osimertinib. To date, there are no approved inhibitors for the treatment of Osimertinib...

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Identifiers

PMID: 37885208
DOI: 10.1021/acs.jmedchem.3c01165

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance.PMID 37885208Read ↗

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CZC54252 overcomes Osimertinib resistance by targeting EGFRC797S mutations.Semantic proximity Read ↗

Recent Progress of Small-Molecule Epidermal Growth Factor Receptor (EGFR) Inhibitors against C797S Resistance in Non-Small-Cell Lung Cancer.Semantic proximity Read ↗

Design, synthesis, and antitumor activity evaluation of potent fourth-generation EGFR inhibitors for treatment of Osimertinib resistant non-small cell lung cancer (NSCLC).Semantic proximity Read ↗

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Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.Semantic proximity Read ↗

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Design and synthesis of 4th generation EGFR inhibitors against human triple (Del19/T790M/C797S) mutation.Semantic proximity Read ↗

Structure-guided discovery of a potent 2-aryl-4-aminoquinazoline-based inhibitor overcoming osimertinib resistance driven by EGFR C797S mutation in NSCLC.Semantic proximity Read ↗

Quinazoline-based fourth-generation EGFR tyrosine kinase inhibitors to overcome C797S-mediated resistance in non-small cell lung Cancer (NSCLC).Semantic proximity Read ↗

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