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Aryl ruthenium complex, preparation method and application thereof

A ruthenium complex and complex technology are applied in the field of aryl ruthenium complexes and preparations, which can solve the problems of no tumor inhibition, cross-drug resistance and the like, and achieve the effects of low cost, easy availability of raw materials and simple preparation method.

Inactive Publication Date: 2013-05-22
GUANGXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the use of cisplatin also has certain shortcomings. It has no inhibitory effect on certain tumors and is prone to cross-resistance with other platinum agents.
In addition, cisplatin has a variety of side effects, such as nephrotoxicity, peripheral neurotoxicity, bone marrow toxicity, hematological toxicity and emetogenicity, etc.

Method used

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  • Aryl ruthenium complex, preparation method and application thereof
  • Aryl ruthenium complex, preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Preparation of Aryl Ruthenium Complexes

[0022] The preparation of aryl ruthenium complex, its specific steps are as follows:

[0023] 0.366g RuCl with ruthenium weight content 37% 3 ·xH 2 O and 3ml of γ-terpinene with a purity of 95% were dissolved in 10ml of ethanol, heated to reflux and stirred for 6 hours. The product A was obtained by standing and precipitating. Weigh 0.091g of thiosemicarbazide and 0.112g of 2-formylthiosemicarbazone and dissolve them together in 5ml of methanol solution, heat to 70°C, and after 3 hours, stand and precipitate to obtain 2-formylthiophene aldehyde thiosemicarbazone. Dissolve 2-formylthiophene aldehyde thiosemicarbazone (47mg, 0.1mmol) and product A (31.5mg, 0.05mmol) in 8ml of dichloromethane, heat at 45°C, stir and reflux for 6 hours, and a reddish-brown solid precipitates out, which is product.

Embodiment 2

[0025] In vitro anti-tumor activity experiment

[0026] In vitro cytotoxicity assays were performed using the MTT method. The aryl ruthenium complex obtained in Example 1 was reacted with gastric cancer cell line SGC7901 and nasopharyngeal cancer cell line CNE-1 for 72 hours respectively, and the results are shown in Table 2.

[0027] The half maximal effective concentration (IC50) of table 2 aryl ruthenium complexes to tumor cell lines

[0028] cell line

[0029] From the results of Example 2, it can be seen that the aryl ruthenium complex of the present invention has strong anti-tumor activity through anti-tumor experiments in vitro. The invention provides a new idea for researching and developing new antitumor drugs.

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Abstract

The invention discloses an aryl ruthenium complex, a preparation method and an application thereof. The aryl ruthenium complex is chemically named as monochlorinate-chlorine-thiophene-2-hydrazine carbothioamide-cymenoruthenium (II). The preparation method comprises the following steps of: 1, dissolving RuCl3.xH2O and gamma-terpinene into ethanol, heating, refluxing and stirring for 6 hours to obtain a product A; 2, dissolving thiosemicarbazide and 2-formylthiophene together in methanol solution, heating to 70 DEG C for 3 hours, standing and separating to obtain 2-formylthiophene thiosemicarbazones; and 3, dissolving the products obtained in steps (1) and (2) into dichloromethane, heating to 45 DEG C, stirring and refluxing for 6 hours to obtain the monochlorinate-chlorine-thiophene-2-hydrazine carbothioamide-cymenoruthenium (II). The aryl ruthenium complex and the preparation method have the beneficial effects that the preparation method is simple, raw materials are easy to obtain, and an advantage of low cost is achieved; and the obtained product is used for preparing medicines for treating cancers, and can be produced into dosage forms such as injection, tablets, pills, capsules, suspension agents or emulsion to use.

Description

technical field [0001] The present invention relates to a kind of aryl ruthenium complex and its preparation method and application, more specifically monochloride monochloro-thiophene-2-formaldehyde thiosemicarbazone-methylcymenyl ruthenium (II) and its preparation method and uses. Background technique [0002] At present, cisplatin has become one of the three most widely used drugs for cancer treatment in the world, with annual sales in the United States reaching nearly 500 million US dollars. However, the use of cisplatin also has certain shortcomings. It has no inhibitory effect on certain tumors and is prone to cross-resistance with other platinum agents. In addition, cisplatin has a variety of side effects, such as nephrotoxicity, peripheral neurotoxicity, bone marrow toxicity, hematological toxicity, and emetogenicity. Therefore, finding new anti-tumor drugs with high efficiency, low toxicity and no cross-resistance has always been a research hotspot for scientific ...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
Inventor 李培源苏炜霍丽妮陈睿
Owner GUANGXI UNIV OF CHINESE MEDICINE
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