Injection medicine composition with synergistic action of vitamin C and benzsulfamide compounds
A technology of benzenesulfonamide and composition, which is applied in the field of pharmaceutical composition for the treatment of malignant tumors, and can solve problems such as poor targeting and large systemic side effects
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[0128] F-1 to F-15 are all known compounds, wherein F-1 to F-11 are obtained from commercial sources (purchased from Beijing Yinuokai Technology Co., Ltd.), and F-12 to F-15 are prepared according to the following general method: Add 4-hydroxybenzenesulfonamide (F-6, 1.73g, 10mmol) and dimethylformamide (20mL) into a 100mL round bottom flask, stir at room temperature until clear, add 60% NaH (0.8g, 20mmol), and Stir for 5 minutes, then add haloalkane (30 mmol), continue stirring at room temperature, and track and detect by TLC. After the reaction is complete, pour the reaction mixture into water, extract with ethyl acetate (100mL×3), combine the ethyl acetate phases, wash with water (100mL×1), wash with saturated brine (100mL×1), and dry over anhydrous sodium sulfate for 6 hours , filtered, the filtrate was concentrated to dryness under reduced pressure, silica gel column chromatography, petroleum ether / ethyl acetate (10:1, 5:1) was eluted sequentially, the target product was ...
experiment example 1、Vc
[0135] Experimental example 1, the inhibitory effect of Vc combined with various benzenesulfonamide compounds on tumor cells
[0136] experimental method
[0137] drug configuration
[0138] Weigh 88 mg of vitamin C (hereinafter referred to as Vc) and dissolve it in 0.5 mL of autoclaved water to make a 1 mol / L stock solution, filter it with a 0.22 μm disposable needle filter in an ultra-clean workbench, and store it in a -80 °C refrigerator , When used, it is directly added to the culture medium to make a corresponding concentration of liquid medicine.
[0139] MTT assay for cell viability
[0140] After the cell lines in the logarithmic growth phase were digested with 0.25% trypsin, the RPMI1640 culture medium containing 10% fetal bovine serum was used to make a single cell suspension, and 3×10 3 Inoculate in a 96-well plate at a density of cells / mL, add 100 μL of cell suspension to each well, and place at 37°C, 5% CO 2 Cultivate in a sterile incubator in an incubator for 2...
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