A tetravalent platinum complex targeting carbonic anhydrase and its preparation method and application
A technology of carbonic anhydrase and tetravalent platinum, which is applied in the direction of platinum-based organic compounds, platinum-group organic compounds, and compounds containing elements of group 8/9/10/18 of the periodic table, etc. and poor specificity to achieve the effect of reducing liver damage, simple preparation method, and broad development space
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Embodiment 1
[0061] Preparation of tetravalent platinum complex targeted by carbonic anhydrase in embodiment 1
[0062] 1. Experimental method
[0063] S1. Dissolve cisplatin (2.0mmol, 600.0mg) in 35.0mL of deionized water, add 12.0mL of 30% hydrogen peroxide (H 2 o 2 ), carry out redox reaction at 65°C for 5h, then react overnight at room temperature, remove H by filtration 2 o 2 , to obtain a pale yellow solid, which is cis-diamine dichlorodihydroxyplatinum (IV);
[0064] S2. Add the cis-diamine dichlorodihydroxyplatinum (IV) (333.0 mg, 1.0 mmol) obtained in step S1 into 3.0 mL of anhydrous dimethyl sulfoxide (DMSO), and add succinic anhydride under magnetic stirring (240.2mg, 2.2mmol), anhydride reaction at 25°C for 24h, after the reaction was completed, 100.0mL of water was added, the solvent was lyophilized, and the solid was washed three times with ice acetone and ice ether to obtain a white solid, namely cis-di Amine dichlorodicarboxy platinum (IV);
[0065] S3. Weigh the cis-...
Embodiment 2
[0074] Example 2 Preparation of tetravalent platinum complex targeted by carbonic anhydrase
[0075] 1. Experimental method
[0076] S1. Dissolve oxaliplatin (795.0mg, 2mmol) in 35.0mL of deionized water, add 12.0mL of 30% H2O under magnetic stirring 2 o 2 , carry out redox reaction at 70°C for 4h, then react overnight at room temperature, remove H by filtration 2 o 2 , to obtain a gray solid, which is cis-oxalic acid (trans-1,2-cyclohexanediamine) dihydroxyplatinum (II);
[0077] S2. Add cis-oxalic acid (trans-1,2-cyclohexanediamine) dihydroxyplatinum (II) (429.3 mg, 1.0 mmol) obtained in step S1 into 3.0 mL of anhydrous DMF, and add under magnetic stirring Succinic anhydride (240.2 mg, 2.4 mmol), reacted at 70°C for 48 hours, after the reaction was completed, 100.0 mL of water was added, the solvent was removed by lyophilization, and the solid was washed three times with ice acetone and ice ether to obtain a brown-gray solid, which was cis - Platinum(IV) oxalate (trans-...
Embodiment 3
[0088] Example 3 Study on the Activity of Complex 1 on Various Tumor Cell Lines
[0089] 1. Experimental method
[0090] Cytotoxicity was determined by the tetrazolium salt (MTT) colorimetric method. Cells were digested with trypsin, collected, and resuspended into a single cell suspension with culture medium, and the cell concentration was adjusted to 5 × 10 by cell counting. 4 / mL, and inoculated in a 96-well culture plate, 160 μL per well, at 37 ° C, containing 5% CO 2 After culturing in the incubator for 24 hours, drugs of different concentrations were added respectively (dosing well: add the complex 1 prepared in Example 1 above; control well: add cisplatin), and continue to incubate for 72 hours. 4 hours before the end, at Add 20 μL MTT (5 mg / mL) to each well, carefully remove the supernatant after 4 hours, add 150 μL DMSO to each well, shake at room temperature for 10 min, and measure the OD value of each well at a wavelength of 595 nm with a microplate reader.
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