Article
Discovery, optimization and biological activity evaluation of genipin derivatives as potential KRAS G12D inhibitors.
Bioorganic chemistry - 1 Jul 2024
Sun Ran, Hu Yangfan, Liu Xiangwen, Lin Yingjun, Lv Dan, Li Wei, Fu Lei, Jiang Faqin
Abstract excerpt
A series of genipin derivatives were designed and synthesized as potential inhibitors targeted KRAS G12D mutation. The majority of these compounds demonstrated potential antiproliferative effects against KRAS G12D mutant tumor cells (CT26 and A427). Notably, seven compounds exhibited the anticancer effects with IC50 values ranging from 7.06 to 9.21 µM in CT26 (KRASG12D) and A427 (KRASG12D) cells and effectively...
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