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Discovery of novel 4-arylamino-quinazoline derivatives as EGFRL858R/T790M inhibitors with the potential to inhibit the non-small cell lung cancers.

Bioorganic chemistry - 1 Oct 2022

Gan Wenhui, Wang Caolin, Pan Qingshan, Li Yuzhen, Guo Yuping, Fan Dang, Peng Yuting, Rao Zixuan, Xu Shan, Zheng Pengwu, Zhu Wufu

Abstract excerpt

Three series of quinazoline derivatives (7a-j, 8a-o, 9a-l) were designed and synthesized as EGFRL858R/T790M inhibitors. Series 7a-j and 8a-o are urea and thiourea derivatives while category 9a-l contain the Michael receptor active warhead. Most of the compounds exhibited excellent anti-proliferative activity in vitro against several cancer cell lines, including non-small cell lung cancer (NSCLC) cell lines A549...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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PMID: 35792314
DOI: 10.1016/j.bioorg.2022.105994

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