Design and Synthesis of alpha,beta-Epoxyketones as New Anticancer Agents

作者：Ma Zhengyue; Zhang Xinghua; Wang Shikui; He Yang; Yang Gengliang^*; Li Beilei; Yang Junjie; Lu Yuejuan; Sun Jiewei

来源：Chinese Journal of Chemistry, 2011, 29(4): 757-764.

DOI：10.1002/cjoc.201190153

• alpha,beta-epoxyketones
• thiochromanones
• anticancer activity
• Darzens condensation reaction

As epoxy functional group has high anticancer activity, alpha,beta-epoxyketones were designed and synthesized as new anticancer agents, and their structures were confirmed by UV, (1)H NMR, IR, MS technigeces and elemental analysis. Their in vitro anticancer activities were evaluated by MTT method and the results showed that the compound 4c exhibited good activity with IC(50) of 17.8, 22.0 and 24.1 mu g/mL against A-549, Hela and HepG2 cells, respectively. The dose of LD50 of the mice by intragastric administration was 1864.4 mg/kg. Therefore, the alpha,beta-epoxyketones could potentially provide as new anticancer agents.

• 出版日期2011-4
• 单位河北大学