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Cyclometalated platinum complex and preparation method thereof

A platinum complex and cyclometal technology, applied in the field of cyclometal platinum complex and its preparation, can solve the problems of drug resistance of cancer cells, damage to healthy cells, etc. Effect

Active Publication Date: 2016-10-12
合肥欧申福德生物科技有限责任公司
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  • Application Information

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Problems solved by technology

In the course of treatment, it will cause great damage to healthy cells, and long-term use will make cancer cells resistant to drugs

Method used

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  • Cyclometalated platinum complex and preparation method thereof
  • Cyclometalated platinum complex and preparation method thereof
  • Cyclometalated platinum complex and preparation method thereof

Examples

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Embodiment Construction

[0034] 1. Add 2.12g (20mmol) benzaldehyde, 6.05g (50mmol) acetophenone and 250mL ethanol in a 500mL round bottom flask, stir at room temperature for 5 minutes, then add 5.60g (100mmol) potassium hydroxide dissolved in a small amount of water, React at room temperature for 12 hours, then add 150mL of 35wt% ammonia water, heat up to 60°C and react for 4 hours; after the reaction, cool to room temperature, filter under reduced pressure, and recrystallize the obtained solid with ethanol to obtain Intermediate 1 as a white powdery solid 3.68g. Yield: 60%. 1 H NMR (400MHz, DMSO) δ8.35(d, J=7.7Hz, 4H), 8.21(s, 2H), 8.06(d, J=7.6Hz, 2H), 7.72–7.45(m, 9H).

[0035] 2. Add 0.40g (1.3mmol) 2,4,6-triphenylpyridine, 0.42g (1.0mmol) potassium chloroplatinite and 50mL acetic acid to a 250mL round bottom flask, and react at 130°C for 3 days. Cool to room temperature after completion, filter with suction, and recrystallize from acetonitrile to obtain the target product Z1, which is a yellow-...

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Abstract

The invention discloses a cyclometalated platinum complex and a preparation method thereof, wherein the cyclometalated platinum complex has the structural formula defined in the specification. With cheap and easily available benzaldehyde, acetophenone and the like as raw materials, an organic ligand is simply and efficiently synthesized and then is subjected to a reaction with potassium chloroplatinite, and the target product-cyclometalated platinum complex is obtained. Property studies indicate that the cyclometalated platinum complex can generate fluorescence enhancement response on proteins and can be applied in developing and imaging of living cells. Cell toxicity tests indicate that the cyclometalated platinum complex has relatively strong killing efficiency on cancer cells-mouse breast cancer cells (4T1), has quite small toxicity on healthy cells-mouse embryonic fibroblasts (3T3). Therefore, the cyclometalated platinum complex has wide application prospect in the field of anticancer drug research.

Description

1. Technical field [0001] This article relates to a cyclometal platinum complex and a preparation method thereof, which is an anticancer drug with strong lethality to cancer cells, low toxicity to healthy cells, and the ability to combine with proteins to increase fluorescence. 2. Background technology [0002] Cancer is one of the most important social problems facing the human world today. Its occurrence is caused by many social or natural problems, such as: population aging, smoking, air pollution, water pollution, etc. How to effectively prevent and treat cancer has become a top priority of scientific research. At present, there are three main methods of clinical treatment of cancer: surgery, radiation therapy and chemotherapy. However, surgical treatment has disadvantages such as large trauma, high risk, and complications; radiation therapy can also damage healthy cells while killing cancer cells, and cancer often recurs within 8-10 months; chemotherapy is the current ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00C09K11/06G01N21/64
CPCC07F15/0086C09K11/06C09K2211/185G01N21/6486
Inventor 田肖和祝英忠张明珠罗坤吴杰颖田玉鹏周虹屏杨家祥李飞李胜利
Owner 合肥欧申福德生物科技有限责任公司
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