Design and Synthesis of α, β-Epoxyketones as New Anticancer Agents  

作　　者：马正月 张兴华 王士奎 何洋 杨更亮 李蓓蕾 杨俊杰 鲁悦娟 孙杰威 

机构地区：[1]Key Laboratory for Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, Heibei 071002, China

出　　处：《Chinese Journal of Chemistry》2011年第4期757-764,共8页中国化学（英文版）

基　　金：Project supported by the National Natural Science Foundation of China （Nos. 20375010, 20675084）, the Hebei Province Programs for Science and Technology Development （Nos. 06276479B, 07276407D）, Key Laboratory for Pharmaceutical Quality Control of Hebei Province Fund （No. 09265631 D-14） and Hebei University Found （No. 2010Q33）.

摘　　要：As epoxy functional group has high anticancer activity, α, β-epoxyketones were designed and synthesized as new anticancer agents, and their structures were confirmed by UV, 1H NMR, IR, MS technigeces and elemental analysis. Their in vitro anticancer activities were evaluated by MTF method and the results showed that the compound 4c exhibited good activity with IC50 of 17.8, 22.0 and 24.1 μg/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 α, β-epoxyketones could potentially provide as new anticancer agents.As epoxy functional group has high anticancer activity, α, β-epoxyketones were designed and synthesized as new anticancer agents, and their structures were confirmed by UV, 1H NMR, IR, MS technigeces and elemental analysis. Their in vitro anticancer activities were evaluated by MTF method and the results showed that the compound 4c exhibited good activity with IC50 of 17.8, 22.0 and 24.1 μg/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 α, β-epoxyketones could potentially provide as new anticancer agents.

关 键 词：α β-epoxyketones thiochromanones anticancer activity Darzens condensation reaction 

分 类 号：O627.42[理学—有机化学] Q513[理学—化学]