Article
Exploration of novel dihydroquinoxalinone derivatives as EGFRL858R/T790M tyrosine kinase inhibitors for the treatment of non-small-cell lung cancer.
Bioorganic chemistry - 1 Jun 2023
Cao Yu, Lu Xixuan, Fu Liping, Shi Tao, Zhang Chong, Zeng Linghui, Zhang Jiankang, Shao Jiaan, Xi Jianjun, Pan Zongfu, Liu Shourong, Zhu Huajian
Abstract excerpt
To overcome or delay the drug-resistance of first-generation epidermal growth factor receptor (EGFR) kinase inhibitors and non-selectivity toxicity mediated by second-generation inhibitors, splicing principle was employed to design and synthesize a series of Osimertinib derivatives containing dihydroquinoxalinone (8-30) as the novel third-generation inhibitors against double mutant L858R/T790M in EGFR. Among...
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