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Ruthenium complex as well as preparation method and use thereof

A technology of ruthenium complexes and ligands, which can be used in ruthenium organic compounds, pharmaceutical formulations, platinum group organic compounds, etc., can solve the problems of cisplatin with large toxic and side effects, achieve good absorption effect, induce tumor cell apoptosis, and be beneficial to The effect of industrial synthesis and preparation

Active Publication Date: 2015-05-27
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is the problem of high toxicity and side effects of cisplatin in the prior art, and further provides a cisplatin with low toxicity and side effects, good drug absorption, strong anticancer activity, strong ability to induce tumor cell apoptosis, and DNA-bonded Strong ruthenium complexes

Method used

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  • Ruthenium complex as well as preparation method and use thereof
  • Ruthenium complex as well as preparation method and use thereof
  • Ruthenium complex as well as preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1 Preparation of ruthenium complexes of the present invention

[0028] The ruthenium complex in this embodiment has the following structure:

[0029]

[0030] The above-mentioned ruthenium complex is synthesized from imidazole as a raw material through a three-step reaction, and the synthetic route is as follows:

[0031]

[0032] In this embodiment, R is -H.

[0033] Its preparation method is specifically:

[0034] (1) Preparation of Compound III

[0035] 1mol imidazole, 2mol K 2 CO 3 1mol benzyl chloride was dissolved in acetone, heated to reflux for 8h, and then the obtained mixed solution was filtered to remove insoluble matter, and the obtained filtrate was spin-dried by a rotary evaporator, and then 10:1 CH 2 Cl 2 with CH 3 OH was used as the eluent for chromatographic column separation to obtain a light yellow solid, which was compound III;

[0036] (2) Preparation of Compound II

[0037] Dissolve 1 mol of compound III obtained in step (...

Embodiment 2

[0041] Embodiment 2 Preparation of ruthenium complexes of the present invention

[0042] The ruthenium complex in this embodiment has the following structure:

[0043]

[0044] The synthetic route of above-mentioned ruthenium complex is identical with embodiment 1. The preparation method of the ruthenium complex described in this example is the same as that in Example 1, the only difference is that in the preparation steps of compound III, benzyl chloride is replaced by 4-methoxybenzyl chloride, and the preparation steps of compound I are as follows: :

[0045] Take 2mol of the NHC ligand shown in formula II and 1mol of Ag 2 O was stirred in 10ml of dichloromethane in the dark for 4 hours, and then added 1mol of dichlorobis(4-methylisopropylphenyl)ruthenium (II), and continued to stir in the dark at 18°C ​​until the reaction was obtained The ruthenium complex.

[0046]

[0047] Among them, R is -OCH 3 .

Embodiment 3

[0048] Embodiment 3 Preparation of ruthenium complexes of the present invention

[0049] The ruthenium complex in this embodiment has the following structure:

[0050]

[0051]The synthetic route of above-mentioned ruthenium complex is identical with embodiment 1. The preparation method of the ruthenium complex described in this example is the same as that in Example 1, the only difference is that in the preparation steps of compound III, benzyl chloride is replaced by 4-methylbenzyl chloride, and the preparation steps of compound I are as follows:

[0052] Take 2mol of the NHC ligand shown in formula II and 1mol of Ag 2 O was stirred in 10ml of dichloromethane in the dark for 4h, then added 1mol of dichlorobis(4-methylisopropylphenyl)ruthenium (II), and continued to stir in the dark at 28°C until the reaction was obtained The ruthenium complex; after the reaction, the above solution was filtered to remove the by-product AgCl, and then 40ml of ether was added to the filtr...

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Abstract

The invention relates to a ruthenium complex, the structural formula of which is shown in a formula I. Compared with cis-platinum, the ruthenium complex provided by the invention is small in toxic and side effects and is good in drug absorption, strong in anti-cancer activity, strong in ability of inducing tumor cell apoptosis and strong in ability of being bonded with DNA, and shows a good function in tumor treatment. The formula is shown in the description.

Description

technical field [0001] The invention relates to a ruthenium complex and belongs to the technical field of antitumor drugs. Background technique [0002] At present, there are three main means of cancer treatment: surgery, radiotherapy and chemotherapy. In the field of chemotherapy (drug therapy), the discovery of the anti-tumor activity of cisplatin (cisplatin dichlorodiammine) is of great significance. Now, cisplatin Platinum has become one of the most widely used drugs in the clinical treatment of testicular cancer, ovarian cancer, head and neck tumors, and bladder cancer. However, the toxic and side effects of cisplatin are also very obvious, such as nephrotoxicity, bone marrow toxicity, ototoxicity, peripheral neurotoxicity, emetic, drug resistance caused by long-term use, etc., and platinum drugs do not work on many tumors. These have limited the application of cisplatin. [0003] In recent years, the research on non-platinum metal-based antitumor drugs is very active...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCC07F15/0046
Inventor 林建国吕高超邱玲郭刘斌杨慧王腾飞
Owner JIANGSU INST OF NUCLEAR MEDICINE
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