Ruthenium complex nano-scale particle, preparation method and application thereof, and anti-tumor drug

A ruthenium complex, nano-scale technology, applied in the field of ruthenium complex nano-scale particles and its preparation, can solve the problem that the ring metal ruthenium complex cannot be used directly, and achieve the effect of good self-assembly function and good conjugation effect

Active Publication Date: 2021-10-15
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

[0005] Aiming at the problems that current ring metal ruthenium complexes cannot be self-assembled to form nanoscale drugs and can be used directly, the present invention provides a nanoparticle and a preparation method thereof

Method used

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  • Ruthenium complex nano-scale particle, preparation method and application thereof, and anti-tumor drug
  • Ruthenium complex nano-scale particle, preparation method and application thereof, and anti-tumor drug
  • Ruthenium complex nano-scale particle, preparation method and application thereof, and anti-tumor drug

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preparation example Construction

[0057] The embodiment of the present invention also provides a preparation method of the above-mentioned ruthenium complex nanoparticles, which includes the following steps:

[0058] (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;

[0059] Wherein, the general formula of compound A is:

[0060] ...(II),

[0061] 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;

[0062] The general formula of the compound B is:

[0063] ...(III);

[0064] 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;

[0065] The general formula of the compound C is:

[0066] .....

Embodiment 1

[0089] A preparation method for ruthenium complex nanoscale particles, comprising the following steps:

[0090] (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:

[0091] .

[0092] (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:

[0093] .

[0094] (3) the R 3 The reactants C...

Embodiment 2

[0107] 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.

[0108] 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: Image 6 , Figure 7 shown.

[0109] from Image 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.

[0110] 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 relative...

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Abstract

The invention relates to the technical field of anti-tumor drugs, and particularly provides ruthenium complex nanoscale particles, a preparation method and application thereof and an anti-tumor drug. The ruthenium complex nano-scale particle is used for a nano-drug and is formed by self-assembly of a ring metal ruthenium complex; the cyclometalated ruthenium complex has a general formula as shown in a formula I. The ruthenium complex nano-scale particles have anti-tumor biological activity, and can be used as an active component of an anti-tumor drug or directly used as the anti-tumor 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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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硕
Owner THE SEVENTH AFFILIATED HOSPITAL SUN YAT SEN UNIV SHENZHEN
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