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Low-toxicity Pt complex and preparation method and application thereof

A complex and low-toxicity technology, applied in platinum group organic compounds, chemical instruments and methods, platinum-based organic compounds, etc., can solve the problems of poor tumor targeting and strong side effects

Active Publication Date: 2021-07-06
江苏南创化学与生命健康研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Platinum drugs are one of the most important chemotherapy drugs, occupying an important market share. However, their defects such as poor tumor targeting and strong side effects have seriously affected their clinical efficacy. For example, cisplatin has severe nephrotoxicity. How to reduce The toxic and side effects of platinum-based drugs is an important hotspot in the research of platinum-based drugs

Method used

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  • Low-toxicity Pt complex and preparation method and application thereof
  • Low-toxicity Pt complex and preparation method and application thereof
  • Low-toxicity Pt complex and preparation method and application thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0037] Preparation of compound c1:

[0038] Add 3.00 g of cisplatin (10.00 mmol) into 180 mL of hydrogen peroxide (30%-35%) solution, avoid light, heat up to 75°C for 7 h, cool down to room temperature, refrigerate overnight, filter, The filter cake was washed with a small amount of cold water, the solid was collected and evaporated to dryness under reduced pressure to obtain 2.90 g of compound c1 as a yellow solid with a yield of 87%.

Embodiment 1

[0040] A kind of low toxicity Pt (IV) complex, its preparation method comprises the steps:

[0041]

[0042] Add 1.00 g of compound a1 (3.90 mmol) and 0.37 g of chloroacetic acid (4.29 mmol) into 10 ml of ethanol solution, add 0.31 g of sodium hydroxide aqueous solution (10 ml) dropwise under ice-cooling, after the addition is complete, heat up to 65°C and react overnight , after the TLC detection reaction is complete, add ethyl acetate to wash twice, adjust the aqueous phase to pH 4-5 with aqueous citric acid, extract twice with ethyl acetate, combine the organic phases, dry the organic phases with anhydrous sodium sulfate, and filter , and evaporated to dryness under reduced pressure to obtain 1.0 g of white solid compound a with a yield of 81%;

[0043] 1 H-NMR (400 MHz, CDCl3): δ (ppm) 7.47 (d, J = 8.5 Hz, 2H), 7.03 (d, J = 16.2 Hz, 1H), 6.97-6.92 (m, 3H), 6.65 (d , J = 2.2 Hz, 2H), 6.36 (d, J = 2.4Hz, 1H), 4.70 (s, 2H), 3.83 (s, 6H).

[0044](2) 0.80 g of compound a...

Embodiment 2

[0050] A kind of low toxicity Pt (IV) complex, its preparation method comprises the steps:

[0051] 283 mg of compound c1 (0.85 mmol) was mixed with 10 mL of dry DMF, and 800 mg of compound a (2.55 mmol), 257 mg of triethylamine (2.55 mmol) and 817 mg of TBTU (2.55 mmol) were added in sequence, and the addition was completed at room temperature. Stirred for 48 h, after the reaction was over, the reaction solvent was concentrated to about 5 mL, methanol was added for crystallization, filtered, the filter cake was washed twice with methanol, and dried under reduced pressure to obtain a pale yellow solid, complex 2; 1 H NMR, 13 The resulting pale yellow solid product was characterized by C NMR and MS, and the data obtained are as follows:

[0052] 1 H-NMR (400 MHz, DMSO-d6): δ (ppm) 7.51 (d, J = 8.8 Hz, 2H ), 7.22 (d, J = 16.3, 1H), 7.03 (d, J = 16.4, 1H), 6.95(d, J = 8.7 Hz, 2H), 6.75(d, J= 2.2 Hz, 2H), 6.62(br, 6H), 6.36(s, 1H), 4.66(s, 2H) , 3.78(s, 6H) ).

[0053] 13 ...

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Abstract

The invention discloses a low-toxicity Pt complex, and belongs to the technical field of anticancer chemical drugs. The structure of the complex is as shown in a general formula (1) or a general formula (2), pterostilbene is introduced into the platinum (IV) complex, and the anti-tumor effect of the platinum complex is improved and the toxic and side effects of the platinum complex on normal cells are reduced by utilizing the anti-inflammatory and anti-oxidation double functions of the pterostilbene.

Description

technical field [0001] The invention relates to the technical field of anticancer chemical drugs, in particular to a low-toxicity Pt(IV) complex and its preparation method and application. Background technique [0002] Tumor treatment is a huge challenge for human beings. At present, tumor treatment mainly adopts three methods: surgery, chemotherapy and radiotherapy. Among them, chemotherapy has a remarkable effect and has the characteristics of high efficiency and broad spectrum. It is widely used in the treatment of various cancers, especially advanced cancers. Platinum drugs are one of the most important chemotherapeutic drugs, occupying an important market share. However, their defects such as poor tumor targeting and strong side effects have seriously affected their clinical efficacy. For example, cisplatin has severe nephrotoxicity. How to reduce The toxic and side effects of platinum-based drugs is an important hotspot in the research of platinum-based drugs. [0003...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0093
Inventor 周文斌颜莉郭子建王晓勇
Owner 江苏南创化学与生命健康研究院有限公司
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