Dinuclear organic metal ruthenium compound and preparation method and application thereof

A technology of organometallic and ruthenium compounds, applied in the field of binuclear organometallic ruthenium compounds and their preparation, achieving the effects of simple preparation methods, readily available raw materials, and low cost

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

The present invention uses thiosemicarbazide as the main ligand to prepare a dinuclear organometallic ruthenium compound, which has strong antitumor activity and has not been reported so far

Method used

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  • Dinuclear organic metal ruthenium compound and preparation method and application thereof
  • Dinuclear organic metal ruthenium compound and preparation method and application thereof
  • Dinuclear organic metal ruthenium compound and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0026] Preparation of Binuclear Organometallic Ruthenium Compounds

[0027] The preparation of binuclear organometallic ruthenium compound, its concrete steps are as follows:

[0028] 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 0.12ml of benzaldehyde and dissolve them in 10ml of 50% ethanol solution, heat to 80°C, and after 4 hours, stand still to precipitate benzaldehyde thiosemicarbazone. Dissolve p-hydroxybenzaldehyde thiosemicarbazone (21mg, 0.1mmol) and product A (32mg, 0.05mmol) in 6ml of acetone, heat at 45°C, stir and reflux for 6 hours, and a red solid is precipitated, which is the product.

Embodiment 2

[0030] In vitro anti-tumor activity experiment

[0031] In vitro cytotoxicity assays were performed using the MTT method. The binuclear organometallic ruthenium compound obtained in Example 1 was reacted with gastric cancer MGC-803 cell line for 72 hours respectively, and the results are shown in Table 2.

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

[0033] cell line

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

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Abstract

The invention discloses a dinuclear organic metal ruthenium compound and a preparation method and application thereof. The chemical name of the dinuclear organic metal ruthenium compound is di(p-hydroxy benzaldehyde) thiosemicarbazone dimethyl isopropylbenzene diruthenium dichloride (II). The preparation method comprises the following steps of: 1) dissolving RuCl3.xH2O and gamma-terpinene into ethanol and carrying out heating reflux and stirring for six hours to obtain a product A; 2) dissolving thiosemicarbazide and p-hydroxy benzaldehyde into ethanol solution, heating the solution to 80 DEG C, standing for four hours and precipitating out p-hydroxy benzaldehyde thiosemicarbazone; and 3) dissolving the products obtained in the steps 1) and 2) into acetone, heating the solution to 45 DEG C and carrying out stirring and reflux for six hours to obtain the product-di(p-hydroxy benzaldehyde) thiosemicarbazone dimethyl isopropylbenzene diruthenium dichloride (II). The preparation method is simple and is 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 a dual-nuclear organometallic ruthenium compound and its preparation method and use, more specifically dichlorinated di-p-hydroxybenzaldehyde thiosemicarbazone dimethylcumene diruthenium (II) 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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/28A61P35/00
Inventor 苏炜李培源钱全全
Owner GUANGXI TEACHERS EDUCATION UNIV
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