Article
Discovery of novel Quinazoline-based KRAS G12C inhibitors as potential anticancer agents.
Bioorganic & medicinal chemistry - 1 Oct 2022
Li Ling, Zhao Huiting, Peng Xiaopeng, Liu Jin, Mai Ruiyao, Chen Jingxuan, Lin Lin, Chen Ting, Yan Jun, Shi Jiaolong, Chen Jianjun
Abstract excerpt
A series of novel quinazoline analogs were designed and synthesized based on ARS-1620 and LLK-10 (a KRAS inhibitor reported by us recently) as KRAS G12C inhibitors with a 5-nitrofuran-2-carboxylic acid warhead. Most of the newly synthesized compounds exhibited antiproliferative activities similar to or better than ARS-1620 and LLK-10. Among them, compound KS-19 showed the highest activity (IC50 = 460 ∼ 870 nM)...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.