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.
Biomembrane-coated capillaries are prepared by coating different kinds of biomembranes including mice red cell membrane, human red cell membrane and S-180 cell membrane on the inner surface of the capillary, respectively. Effects of immobilized biomembrane amount, pH and biomembrane species on the interactions between drugs and biomembranes have been evaluated. The results showed that the chromatographic retention factor for each drug was essentially related to the amount of immobilized biomembrane, the pH and the type of biomembrane.
