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Ruthenium (II) polypyridine complex and preparation method and application thereof

A technology of complexes and polypyridines, applied in the direction of ruthenium organic compounds, platinum group organic compounds, medical preparations containing active ingredients, etc., can solve the problems of not having good effects, and achieve low toxicity, high medical potential, and high production efficiency. high rate effect

Inactive Publication Date: 2016-07-06
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, this compound is only used for the search of G4, and it has no good effect on inhibiting telomerase activity and regulating proto-oncogene expression in combination with G-4 quadruplet

Method used

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  • Ruthenium (II) polypyridine complex and preparation method and application thereof
  • Ruthenium (II) polypyridine complex and preparation method and application thereof
  • Ruthenium (II) polypyridine complex and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A ruthenium (II) polypyridine complex, the complex is based on 2-(1,10-phenanthroline-5-yl)-benzimidazole) as the main ligand, and the complex is based on 2,2'-bipyridine As an auxiliary ligand, the chemical formula of the complex is [Ru(bpy) 2 pbi] 2+ , the structural formula of the complex is:

[0042] denoted as a 1 .

[0043] The complex is prepared by the following steps:

[0044] 1. Synthesize ligand pbi (pbi=2-(1,10-Phenanthrolin-5-yl)-benzo[d]imidazole) to obtain a yellow powder: add 0.001mol o-phenylenediamine and 0.001mol 5-aldehyde to a single-necked flask Based on o-phenanthroline and 0.002mol sodium bisulfite, add 3mL DMF to dissolve, and heat to reflux at 150°C for 6 hours to obtain a brown solution with a small amount of precipitation. Adding 30 mL of water to the reaction solution resulted in a large amount of yellow precipitate, which was filtered with suction, washed with water for several times, and dried in vacuo. 0.255 g of yellow powder was...

Embodiment 2

[0070] A ruthenium (II) polypyridine complex, the complex is based on 2-(1,10-phenanthroline-5-yl)-benzimidazole) as the main ligand, and the complex is based on 1,10'-o-phenanthrene Roline is the auxiliary ligand, and the chemical formula of the complex is [Ru(phen) 2 pbi] 2+ , the structural formula of the complex is:

[0071] denoted as a 2 .

[0072] The complex is prepared by the following steps:

[0073]1. Synthesize ligand pbi (pbi=2-(1,10-Phenanthrolin-5-yl)-benzo[d]imidazole) to obtain a yellow powder: add 0.001mol o-phenylenediamine and 0.001mol 5-aldehyde to a single-necked flask Based on o-phenanthroline and 0.002mol sodium bisulfite, add 3mL DMF to dissolve, and heat to reflux at 150°C for 6 hours to obtain a brown solution with a small amount of precipitation. Adding 30 mL of water to the reaction solution resulted in a large amount of yellow precipitate, which was filtered with suction, washed with water for several times, and dried in vacuo. 0.255 g of ...

Embodiment 3

[0085] Adopt the preparation method similar to embodiment 1, specifically comprise the following steps:

[0086] 1. Synthesize ligand pbi (pbi=2-(1,10-Phenanthrolin-5-yl)-benzo[d]imidazole) to obtain a yellow powder: add 0.001mol o-phenylenediamine and 0.001mol 5-aldehyde to a single-necked flask Based on o-phenanthroline and 0.002mol sodium bisulfite, and dissolved in 3mL of DMF, heated to reflux at 120°C for 12 hours to obtain a brown solution with a small amount of precipitation. Add 5 times the solution volume of water to the reaction solution, a large number of yellow precipitates are produced, filter with suction, wash the filter cake with water several times, and dry it in vacuum. 0.255 g of yellow powder was obtained with a yield of 86%.

[0087] 2. Add 6mmol ruthenium trichloride (RuCl 3 ·3H 2 O), 6mmol lithium chloride monohydrate, and 12mmol bipyridyl, dissolved in 10ml DMF, heated to reflux at 130°C for 10 hours under the protection of argon to obtain a solid-li...

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Abstract

The invention relates to ruthenium (II) polypyridine complex.The complex uses 2-(1, 10-phenanthroline monohydrate-5-base)-benzimidazole) as the main ligand and 2, 2'-bipyridine or 1, 10'-phenanthroline as the auxiliary ligand, and the chemical formula of the complex is [Ru(bpy)2pbi]2+ or [Ru(phen)2pbi]2+.A preparation method of the complex includes the steps of firstly, preparing pbi; secondly, synthesizing a ruthenium metal compound with the auxiliary ligand group; thirdly, synthesizing the target ruthenium (II) polypyridine complex; fourthly, using silica gel chromatography column separation to obtain the product.The ruthenium (II) polypyridine complex is used for preparing medicine combining with telomere G-quadruplex to increase the stability of the telomere G-quadruplex.Compared with the prior art, the ruthenium (II) polypyridine complex prepared by the method has the advantages that the ruthenium (II) polypyridine complex can recognize, combine and stabilize the telomere G-quadruplex, inhibit telomerase activity and regulate proto-oncogene expression, and a theoretical foundation is provided for anticancer medicine screening.

Description

technical field [0001] The invention relates to metal complexes, in particular to a ruthenium (II) polypyridine complex and its preparation and application. Background technique [0002] Nucleic acid is the material basis of biological inheritance. The research on nucleic acid not only helps us explore the origin of life, but also is particularly important in solving gene-related diseases. In addition to the traditional double helix structure, there are many non-classical configurations of nucleic acids, the most striking of which is the G-quadruplex (G4) structure, mainly because it is an effective target for people to regulate biological functions through chemical interference. point. G4 is a four-stranded nucleic acid structure, which is formed by the accumulation of G-tetrads formed by Hoogsteen pairing between G bases. This assembly phenomenon is very common in G-rich nucleic acid sequences . Since G-rich sequences are abundant in many functional gene regions (such ...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCC07F15/0053
Inventor 尹盼盼尚英辉姚天明石硕
Owner TONGJI UNIV
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