Article
Design, synthesis and evaluation of 1,2-dihydropyrido[2,3-d]pyrimidine-6‑carbonitrile derivatives as novel covalent inhibitors for the treatment of KRASG12C-mutant NSCLC.
Bioorganic chemistry - 1 Nov 2025
Yang Fang, Li Minxiong, Chen Lingling, Kang Ning, Cao Wei, Feng Xuejin, Tang Lin, Hu Haiyang, Xi Yunlong, Liu Bing, Li Jing, Zhang Lei, Zhang Yingjun
Abstract excerpt
KRASG12C mutation, which is observed in ∼14 % of lung adenocarcinoma cases, has been established as a pivotal therapeutic target in precision oncology approaches. Herein, a novel series of 1,2-dihydropyrido[2,3-d]pyrimidine-6‑carbonitrile derivatives was developed as KRASG12C inhibitors. One representative compound 8 t exhibited remarkable antiproliferative activity against KRASG12C-mutant non-small-cell lung...
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