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 a...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.展开更多
An efficient method for the selective hydrogenation of a series of α,β-epoxyketones to β-hydroxyketones using catalytic amount of two sulfinyl analogues of NAD^＋ model compounds is reported. The lack of any diaste...An efficient method for the selective hydrogenation of a series of α,β-epoxyketones to β-hydroxyketones using catalytic amount of two sulfinyl analogues of NAD^＋ model compounds is reported. The lack of any diastereoselectivity for the formation of β-hydroxyketones with optically pure sulfinyl analogue of NAD^＋ model supports the radical mechanism proposed previously.展开更多
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）.
文摘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.
基金Project supported by the National Natural Science Foundation of China （No. 20072036） and the Specialized Research Fund for the Doctoral Program of Higher Education of China.Acknowledgment We would like to thank Professor Yun-Dong Wu of the Hong Kong University of Science and Technology and Peking University for helpful advice.
文摘An efficient method for the selective hydrogenation of a series of α,β-epoxyketones to β-hydroxyketones using catalytic amount of two sulfinyl analogues of NAD^＋ model compounds is reported. The lack of any diastereoselectivity for the formation of β-hydroxyketones with optically pure sulfinyl analogue of NAD^＋ model supports the radical mechanism proposed previously.
