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Discovery of Novel 5,6-Dihydro-4H-pyrido[2,3,4-de]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases.

Journal of medicinal chemistry - 11 Apr 2024

Yang Leifu, Li Yaxin, Du Yunling, Guo Yan, Guo Zhenke, Liu Baoxiu, Liu Jianglin, Liu Yanfei, Niu Hongdan, Sun Yueming, Yan Henglin, Yang Yajuan, Yu Shannan, Zhang Yifan, Zhang Yuan, Zheng Kun, Zheng Nanqiao, Zhang Xiaoqing, Zhang Qiang, Hu Liming

Abstract excerpt

HER2 mutations were seen in 4% of non-small-cell lung cancer (NSCLC) patients. Most of these mutations (90%) occur as an insertion mutation within the exon 20 frame, leading to the downstream activation of the PI3K-AKT and RAS/MAPK pathways. However, no targeted therapies have yet been approved worldwide. Here a novel series of highly potent HER2 inhibitors with a pyrido[2,3,4-de]quinazoline core were designed...

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PMID: 38518121
DOI: 10.1021/acs.jmedchem.3c02302

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