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Ruthenium complex nanoscale particle, preparation method and application thereof, and antitumor drug

A technology of anti-tumor drugs and ruthenium complexes, which can be used in anti-tumor drugs, ruthenium organic compounds, drug combinations, etc., can solve the problem that cyclometallic ruthenium complexes cannot be used directly, and achieve good self-assembly function and good conjugation effect. Effect

Active Publication Date: 2022-01-14
THE SEVENTH AFFILIATED HOSPITAL SUN YAT SEN UNIV SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the problems that current ring metal ruthenium complexes cannot be self-assembled to form nanoscale drugs and can be used directly, the invention provides a nanoparticle and a preparation method thereof

Method used

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  • Ruthenium complex nanoscale particle, preparation method and application thereof, and antitumor drug
  • Ruthenium complex nanoscale particle, preparation method and application thereof, and antitumor drug
  • Ruthenium complex nanoscale particle, preparation method and application thereof, and antitumor drug

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preparation example Construction

[0058] The embodiment of the present invention also provides a preparation method of the above-mentioned ruthenium complex nanoparticles, which includes the following steps:

[0059] (1) Provide compound A represented by general formula II, ruthenocene, compound B represented by general formula II and compound C represented by general formula III;

[0060] Wherein, the general formula of compound A is:

[0061] ...(II),

[0062] R 1 Including any one of hydrogen atom, methyl group, phenyl group, bromine group, chlorine group, amino group, carboxyl group, hydroxyl group, aldehyde group, and alkyl group with 2 to 9 carbon atoms;

[0063] The general formula of the compound B is:

[0064] ...(III);

[0065] R 2 Including any one of hydrogen atom, methyl group, phenyl group, bromine group, chlorine group, amino group, carboxyl group, hydroxyl group, aldehyde group, and alkyl group with 2 to 9 carbon atoms;

[0066] The general formula of the compound C is:

[0067] .....

Embodiment 1

[0090] A preparation method for ruthenium complex nanoscale particles, comprising the following steps:

[0091] (1) the R 1 The reactant A1 which is a hydrogen atom and ruthenocene were dissolved in acetonitrile in an equimolar ratio, and refluxed for 24 hours, filtered and collected the solution part, and used a mixture of acetonitrile and toluene with a ratio of 1:20 as the eluent in the Separation and purification on the silica gel column to obtain the product RuA1, the whole reaction is as follows:

[0092] .

[0093] (2) the R 2 The reactants B1 and RuA1 which are hydrogen atoms were dissolved in dichloromethane in equal proportions and reacted under reflux for 24 h, filtered and collected the solution part, and used the mixture of acetonitrile and dichloromethane at a ratio of 1:100 as the eluent in the Separation and purification on a silica gel column to obtain the product RuB1, the whole reaction is as follows:

[0094] .

[0095] (3) the R 3 The reactants C...

Embodiment 2

[0108] The preparation method of this embodiment is the same as that of Example 1, the difference is that in this embodiment, R 1 The substituents are hydrogen, R 2 The substituents are methyl, R 3 The substituent of is hydrogen, and the product obtained is RuZ2.

[0109] RuZ2 was characterized by transmission electron microscopy and scanning electron microscopy. The model of the transmission electron microscope is FEI TecnaiG2 F30, and the accelerating voltage is 200 kV-300 kV; the model of the scanning electron microscope is GeminiSEM500, and the accelerating voltage is 20V-30kV. The results are as follows: Figure 6 , Figure 7 shown.

[0110] From Figure 6 It can be seen that the size of RuZ2 nanoparticles under the transmission electron microscope is relatively uniform and has a small particle size.

[0111] From Figure 7 It can be seen that the size of RuZ2 nanoparticles under the scanning electron microscope is relatively uniform, and the particle size is relati...

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Abstract

The invention relates to the technical field of antitumor drugs, and specifically provides a ruthenium complex nanoscale particle, a preparation method and application thereof, and an antitumor drug. The ruthenium complex nano-scale particles are used for nano-medicine, and are self-assembled by the ring metal ruthenium complex; the ring metal ruthenium complex has a general formula as shown in formula I. The ruthenium complex nanometer particle of the invention has antitumor biological activity, and can be used as an active ingredient of an antitumor drug or directly as an antitumor drug.

Description

technical field [0001] The invention belongs to the technical field of antitumor drugs, and in particular relates to a ruthenium complex nanoscale particle, a preparation method and application thereof, and an antitumor drug. Background technique [0002] Cancer is one of the major diseases that kill human beings. At present, chemotherapy drugs are mainly used to treat cancer. However, because most of the current chemotherapy drugs have serious side effects and drug resistance, the treatment effect is not satisfactory. Therefore, it is urgent to develop new types of drugs. Chemotherapy drugs. [0003] Metal ruthenium complexes have attracted widespread attention because of their good anti-tumor activity. Currently, four cases of metal ruthenium complexes have entered clinical research as anti-tumor agents, and two are in the process of clinical research. Although numerous ruthenium complexes such as Ru1, Ru2, Ru3, Ru4, etc. shown below have been reported to have anti-tumor ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61K31/28A61P35/00
CPCC07F15/0046A61P35/00
Inventor 曾乐立李佳潘逸航张常华巢晖廖国龙方烁
Owner THE SEVENTH AFFILIATED HOSPITAL SUN YAT SEN UNIV SHENZHEN
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