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Binuclear platinum (II) complex as well as preparation method and application thereof

A complex, binuclear platinum technology, applied in the field of binuclear platinum (II) complexes and their preparation, can solve the problems of DNA conformation and function damage, difficult self-repair and intolerance of tumor cells, and achieve superior inhibition of MCF-7 Effects of cell proliferation, complex stability, and crystal availability

Inactive Publication Date: 2013-12-25
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, platinum-based antitumor drugs have become an indispensable drug in tumor treatment. In addition to cisplatin, many anti-tumor platinum-based drugs such as carboplatin, oxaliplatin, and nedaplatin have been used in clinical practice. In the course of clinical use, they also show greater toxicity and certain drug resistance. These shortcomings limit their wider use to a certain extent. Therefore, it is still of great significance to develop new platinum-based antineoplastic drugs.
[0004] In recent years, binuclear platinum complexes have begun to be used as anti-tumor drugs. Studies have shown that such complexes have good anti-tumor activity in vitro. They can bind to the DNA of tumor cells in a variety of ways. The damage is also more serious, making it more difficult for tumor cells to repair themselves and be more difficult to tolerate. It is a class of new drugs with important development and application prospects, and is also one of the important directions for the development of platinum-based antitumor drugs. The binuclear platinum ( II) The structure of the complex has not been reported at home and abroad

Method used

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  • Binuclear platinum (II) complex as well as preparation method and application thereof
  • Binuclear platinum (II) complex as well as preparation method and application thereof
  • Binuclear platinum (II) complex as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Preparation and characterization of complexes:

[0021] (1) The premise ligand 3-alkyl-4-amino-5-mercapto-1,2,4-triazole (the alkyl groups are methyl, ethyl and propyl, respectively) was prepared according to the literature method.

[0022] (2) Synthesize 5-chlorosalicylaldehyde acetal-3-alkyl-4-amino-5-mercapto-1,2,4-triazole Schiff base ligand according to the literature method. Elemental analysis and determination of 5-chlorosalicylaldehyde-3-methyl-4-amino-5-mercapto-1,2,4-triazole Schiff base compound: C 10 h 9 ClN 4 OS, theoretical values ​​(%) in brackets: C, 44.78 (44.70); H, 3.35 (3.38); N, 21.02 (20.85).

[0023] Elemental analysis and determination of 5-chlorosalicylaldehyde-3-ethyl-4-amino-5-mercapto-1,2,4-triazole Schiff base compound: C 11 h 11 ClN 4 OS, theoretical values ​​(%) in brackets: C, 46.67 (46.73); H, 4.02 (3.92); N, 19.76 (19.82).

[0024] Elemental analysis and determination of 5-chlorosalicylaldehyde-3-propyl-4-amino-5-mercapto-1,2,4-t...

Embodiment 2

[0034] Example 2 In vitro anti-tumor activity determination of the binuclear platinum (II) complex of the present invention

[0035] Incubate human breast cancer cells (MCF-7) in medium containing 10% fetal calf serum at 37°C, 5% CO 2 cultured in an incubator, and the MTT method was used to detect the effect of the binuclear platinum (II) complex of the present invention on the proliferation of MCF-7 cells. In the experiment, MCF-7 cells in the logarithmic growth phase were digested and collected by centrifugation to prepare 1 mL of cell suspension. Dilute to a cell density of approximately 1×10 -4 cells / mL of cell suspension, evenly inoculated in a 96-well plate, 200 μL per well, and placed the 96-well plate in CO 2 Incubate in an incubator until the cell monolayer is confluent to the bottom of the wells, add 5 binuclear platinum (II) complexes with gradient concentrations, and set 6 duplicate wells for each group. Cells continue in CO 2 After incubating in the incubator ...

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Abstract

The invention provides a binuclear platinum (II) complex and a preparation method thereof as well as an application thereof as an anti-tumor drug. The binuclear platinum (II) complex provided by the invention is a 5-chlorosalicylaldehyde-3-alkyl-4-amino-5-thio-1,2,4-triazole Schiff base binuclear platinum (II) complex. The preparation method comprises the following steps: dissolving a 5-chlorosalicylaldehyde-3-alkyl-4-amino-5-thio-1,2,4-triazole Schiff base ligand in absolute methanol, dropwise adding triethylamine by equal molar weight, dropwise adding a water solution of potassium tetrachloroplatinate (II) by equal molar weight to an absolute methanol solution of the ligand, stirring, and separating out a solid product. According to the complex, a synthesis method is simple, the structure is simple, and crystals are easily obtained; a cytology test shows that the complex has a remarkable inhibition effect for human cancer cells and can be applied to the preparation of anti-tumor drugs.

Description

technical field [0001] The invention relates to a binuclear platinum (II) complex, in particular to a binuclear platinum (II) complex and its preparation method and application. Background technique [0002] Malignant tumors are one of the major diseases that seriously threaten human health and life. In recent years, due to the influence of factors such as environmental deterioration, bad living habits, and population aging, the incidence of malignant tumors has shown an obvious upward trend. Malignant tumors have become an urgent problem for humans to overcome. As one of the most serious medical problems, the research of antineoplastic drugs has been listed as one of the most important strategic issues in the development of new drugs in my country. [0003] Since cisplatin was approved as a drug for clinical treatment of tumors in 1978, research on the application of metal complexes, especially platinum compounds, in the medical field has developed rapidly. At present, plat...

Claims

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Application Information

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IPC IPC(8): C07D249/12A61P35/00
Inventor 袁彩霞朱苗力卢丽萍
Owner SHANXI UNIV
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