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A novel platinum complex, preparation method and use

A technology for platinum complexes and uses, which is applied in the field of platinum complexes with anticancer activity and their preparation, can solve problems such as violent reactions of platinum complexes, and achieve the effects of mild conditions, stable product properties, and easy mass production and production.

Inactive Publication Date: 2011-11-30
WUHAN KATYGEN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In addition, in the synthesis process of existing platinum complexes, the temperature is relatively high (30°C-80°C) and the reaction is relatively violent, which needs to be improved.

Method used

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  • A novel platinum complex, preparation method and use
  • A novel platinum complex, preparation method and use
  • A novel platinum complex, preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 Synthesis of platinum complexes of the present invention-polyarginine platinum complexes

[0040] (1) Synthesis of polyarginine

[0041] Experimental instruments and materials:

[0042] Dimethylformamide (DMF), piperidine, resin, dichloromethane (DCM), Kaiser kit, 1-hydroxybenzotriazole (HOBt), tetramethyluronium hexafluorophosphate (HBTU), diiso Propylethylamine (DIEA), methanol, various amino acids, and peptide solid-phase synthesis tubes.

[0043] Experimental steps:

[0044] Weigh the resin and put it into the peptide solid-phase synthesis tube (hereinafter referred to as the reactor), and add an appropriate amount of DMF to swell for 10 minutes. DMF was removed for Fmoc deprotection reaction, that is, an appropriate amount of DMF solution containing 20% ​​piperidine was added, fully stirred, the solution was removed after 5 minutes, and 20% piperidine DMF solution was added again for 7 minutes for deprotection. Remove the protection solution, wash ...

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PUM

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Abstract

The invention discloses a platinum complex and its preparation method and application. The structural formula of the platinum complex is shown in formula I, wherein, R is a polypeptide. The platinum complex of the present invention has a stable structure, and the cytological test shows that the inhibitory effect of the platinum complex of the present invention on human colon cancer HCT-116 cells is significantly stronger than that of oxaliplatin on human colon cancer HCT-116 cells. The results show that the platinum complex of the present invention has a significant inhibitory effect on tumor cells, and can be used as a drug for treating and preventing cancer.

Description

technical field [0001] The invention relates to a platinum complex, in particular to a platinum complex with anticancer activity and a preparation method thereof, belonging to the field of platinum complexes. Background technique [0002] Since the discovery of cisplatin's anticancer activity in 1967, the application and research of platinum-based metal anticancer drugs have developed rapidly. Today, this class of drugs has become an indispensable drug in cancer chemotherapy. In 1995, the World Health Organization evaluated nearly 100 anticancer drugs in the world, and the comprehensive evaluation scores of cisplatin, such as curative effect and market, ranked among the top. According to statistics, in my country's anti-cancer chemotherapy regimens, cisplatin-based or cisplatin-based regimens account for 70% to 80% of all chemotherapy regimens. The achievements of cisplatin and carboplatin have greatly encouraged scholars from all over the world to study better and more ef...

Claims

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Application Information

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IPC IPC(8): C07K5/08C07K5/10C07K7/06C07K7/08C07K1/20A61K38/06A61K38/07A61K38/08A61K38/10A61P35/00
Inventor 陈建华黄毅熊俊宇陈彩虹
Owner WUHAN KATYGEN PHARMA