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

• Published in: Chinese journal of chemistry Vol. 29; no. 4; pp. 757 - 764
• Main Author: 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
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 01.04.2011; WILEY‐VCH Verlag; Wiley
• Subjects: anticancer activity; Chemistry; Chemistry, Multidisciplinary; Darzens condensation reaction; Hela; HepG2细胞; IC50; Physical Sciences; Science & Technology; thiochromanones; α,β‐epoxyketones; β-epoxyketones; 元素分析; 抗癌活性; 抗癌药物; anticancer activity; ARENE OXIDES; alpha,beta-epoxyketones; thiochromanones; Darzens condensation reaction
• ISSN: 1001-604X; 1614-7065
• DOI: 10.1002/cjoc.201190153

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.