9-Chlorofluorene reacted with aromatic aldehydes and ketones in the presence of phase transfer catalyst, giving the Darzens condensation epoxy products.
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
文摘9-Chlorofluorene reacted with aromatic aldehydes and ketones in the presence of phase transfer catalyst, giving the Darzens condensation epoxy products.
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.
