Article
Discovery of ARS-1620 analogs as KRas G12C inhibitors with high in vivo antitumor activity.
Bioorganic chemistry - 1 Apr 2022
Zhao Huiting, Li Ling, Liu Jin, Mai Ruiyao, Chen Jingxuan, Chen Jianjun
Abstract excerpt
KRas is the most frequently mutated protein of the three Ras isoforms in various cancer types. KRas mutations (i.e. G12C) are present in approximately 30% of human cancers. Based on our previously reported KRas G12C inhibitor LLK-10, we designed a series of quinazoline analogues with a trifluoromethacrylic acid warhead as covalent inhibitor of KRas G12C. The pharmacological activities of these compounds were...
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