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Organic metal ruthenium compound and preparation method and application thereof

A ruthenium compound and organometallic technology is applied in the field of organometallic ruthenium compounds and their preparation, and achieves the effects of low cost, readily available raw materials and simple preparation method

Inactive Publication Date: 2013-03-13
GUANGXI TEACHERS EDUCATION UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Organometallic ruthenium compounds were prepared with curcuminoids as the main ligands. Due to the synergistic effect of metal ruthenium and curcuminoids ligands, their anti-tumor activity can be enhanced. No relevant reports have been seen so far.

Method used

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  • Organic metal ruthenium compound and preparation method and application thereof
  • Organic metal ruthenium compound and preparation method and application thereof
  • Organic metal ruthenium compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation of organometallic ruthenium compounds

[0026] The preparation of organometallic ruthenium compound, its concrete steps are as follows:

[0027] 1) 0.366g ruthenium weight content is 37% RuCl 3 ·xH 2 O and 3ml of γ-terpinene with a purity of 95% were dissolved in 10ml of absolute ethanol, heated and stirred under reflux for 6 hours. The product A was obtained by standing and precipitating. 2) Weigh 0.091g of acetylacetone and 0.12ml of thiophene formaldehyde and dissolve them in 10ml of ethanol solution with a concentration of 50% by volume, heat to 80°C, and after 4 hours, let it stand for precipitation to obtain 1,7-di-2-thiophene -1,6-Heptadiene-3,5-dione.

[0028] 3) Dissolve 20mg, 0.2mmol of 1,7-di-2-thiophene-1,6-heptadiene-3,5-dione (20mg, 0,2mmol) and 32mg, 0.05mmol of product A in 8ml without Water and ethanol, heated and stirred to reflux for 6 hours, after the reaction was completed, the solution was evaporated to leave 2ml of liquid, and 30m...

Embodiment 2

[0030] In vitro anti-tumor activity test:

[0031] In vitro cytotoxicity assays were performed using the MTT method. The organometallic ruthenium compound obtained in Example 1 was reacted with gastric cancer SGC 7901 cell line for 72 hours respectively, and the results are shown in Table 2.

[0032] Table 2 The half maximal effective concentration (IC) of organometallic ruthenium compounds to tumor cell lines 50 )

[0033] cell line

[0034] From the results of Example 2, it can be seen that the organometallic ruthenium compound of the present invention has a strong anti-tumor activity through in vitro anti-tumor experiments. The invention provides a new idea for researching and developing new antitumor drugs.

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Abstract

The invention discloses an organic metal ruthenium compound and a preparation method and application thereof. The chemical name of the organic metal ruthenium compound is 1,7-bi-2-thiophene-1,6-heptadiene-3,5-diketone-methyl isopropylbenzene ruthenium chloride (II). The preparation method comprises the following steps of: 1) dissolving RuCl3.xH2O and gamma-terpinene into ethanol, carrying out heating reflux and stirring for six hours to obtain a product A; 2) dissolving acetylacetone and thiophenecarboxaldehyde into ethanol solution, heating the solution to 80 DEG C, standing for four hours and precipitating out 1,7-bi-2-thiophene-1,6-heptadiene-3,5-diketone; and 3) dissolving the products obtained in the steps 1) and 2) into absolute ethyl alcohol and carrying out heating, stirring and reflux for six hours to obtain the product-1,7-bi-2-thiophene-1,6-heptadiene-3,5-diketone-methyl isopropylbenzene ruthenium chloride (II). The preparation method is simple and low in cost; raw materials are easily available; and the obtained product is used for preparing the drugs for treating cancers and can be prepared into injections, tablets, pills, capsules, suspending agents or emulsion.

Description

technical field [0001] The present invention relates to an organometallic ruthenium compound and its preparation method and use, more specifically to an organometallic ruthenium compound and its preparation method and use. 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 researchers. [0003] One of the important research ideas is ...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/381A61P35/00A61P1/00
Inventor 苏炜黄初升李培源雷晓琳
Owner GUANGXI TEACHERS EDUCATION UNIV
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