Article
Design, synthesis, and evaluation of 4(1H)-quinolinone and urea derivatives as KRASG12C inhibitors with potent antitumor activity against KRAS-mutant non-small cell lung cancer.
European journal of medicinal chemistry - 15 Dec 2022
Cheng Rongjie, Lv Xiashi, Bu Huagang, Xu Qiaoliang, Wu Jianzhuang, Xie Kexin, Tang Jiaqi, Wang Lei, Zhuang Jian, Zhang Yihua, Zhang Yaliang, Yan Chao, Lai Yisheng
Abstract excerpt
KRASG12C is the most prevalent KRAS mutation in non-small cell lung cancer (NSCLC) and has emerged as a promising therapeutic target. Herein, two series of novel 4(1H)-quinolinone and urea compounds were designed based on the reported KRASG12C inhibitor SH-9. Many compounds showed significantly growth inhibitory activity against human NSCLC cells with KRASG12C mutation in cell viability assays. Compound 20a...
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