Pt (II) complex with anti-tumor activity as well as preparation method and application of Pt (II) complex
A technology of anti-tumor activity and complexes, applied in the field of biomedicine, can solve the problems that have not been fully elucidated, the complex mechanism of cisplatin resistance, etc., and achieve the effects of variable structure, environmental friendliness and convenient synthesis
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[0054] A preparation method of a Pt(II) complex with antitumor activity, comprising the following steps:
[0055] In the organic solvent acetonitrile or acetone, add benzothiazole-functionalized imidazolium salt ligand and silver oxide at a molar ratio of 2:1, react for 4-6 hours at 50°C in the dark, filter, and add Pt(COD ) Cl 2 , the molar ratio between it and the imidazolium salt ligand functionalized with benzothiazole is 1:1, continue to react at room temperature for 2-4 hours, filter, and obtain light yellow blocky crystals by ether volatilization method, which is the Pt(II) complex.
[0056] The application of Pt(II) complexes Pt1, Pt2, Pt3 and Pt4 with anti-tumor activity in the preparation of anti-tumor drugs, the specific application method is as follows: Take cancer cells in the growth phase, digest them with trypsin, seed the plate, and incubate at 37°C for 24h To make the cells adhere to the wall, add different concentrations of benzothiazole-functionalized azacy...
specific Embodiment 1
[0058] Specific embodiment one: (preparation and performance of Pt (II) complex Pt1), reaction equation is as follows:
[0059]
[0060] At 50°C, add the ligand HL 1 PF 6 87.4mg (0.2mmol), acetonitrile 5mL, silver oxide 23mg (0.1mmol), react for 4 hours, and filter. Add Pt(COD)Cl to the filtrate 2 74.8mg (0.2mmol), continued to react at room temperature for 2 hours, centrifuged, concentrated the filtrate to 2mL, added diethyl ether to precipitate a yellow solid, washed the yellow solid twice with diethyl ether, then dissolved it with acetonitrile, slowly added diethyl ether, and recrystallized to obtain 73 mg of benzene And thiazole-functionalized nitrogen-heterocyclic carbene ligand-coordinated platinum compound Pt1, the yield was 48%. Ether volatilization method to obtain the crystal of Pt1 compound, the single crystal structure is as figure 1 shown.
[0061] Pt1 compound, physical and chemical properties are: light yellow crystal, easily soluble in acetonitrile, DMS...
specific Embodiment 2
[0062] Specific embodiment two: (Pt (II) complex PtPreparation and performance), reaction equation is as follows:
[0063]
[0064] At 50°C, add the ligand HL 1 PF 6 87.4mg (0.2mmol), acetonitrile 5mL, silver oxide 23mg (0.1mmol), react for 4 hours, and filter. Add Pt(COD)Cl to the filtrate 2 74.8mg (0.2mmol) and 18mg (0.3mmol) of acetic acid, continue to react at 50°C for 2 hours, centrifuge and filter, concentrate the filtrate to 2mL, add diethyl ether to precipitate a yellow solid, wash the yellow solid twice with diethyl ether, then dissolve it with acetonitrile, slowly Diethyl ether was added and recrystallized to obtain 53 mg of benzothiazole-functionalized nitrogen-heterocyclic carbene ligand-coordinated platinum compound Pt2, with a yield of 39%. Ether volatilization method obtains the crystal of Pt2 compound, single crystal structure such as figure 2 shown.
[0065] The physical and chemical properties of Pt2 compound are: light yellow crystal, easily soluble...
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