Benzisothiazole derivatives as KRAS G12C inhibitors for potential treatment of non-small cell lung cancer.
KRAS G12C mutation is a key driver of multiple solid tumors, and has recently become a crucial target for therapy via small molecules that covalently bind to the mutated cysteine. Herein, a series of benzisothiazole derivatives is presented as KRAS G12C inhibitors utilizing a scaffold-hopping strategy. Among them, S32...