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Synthesis method and application of ruthenium (II) polypyridine metal complex with anti-tumor effect

A technology of metal complexes and synthesis methods, which can be used in antitumor drugs, ruthenium organic compounds, platinum group organic compounds, etc., and can solve problems such as restricted use

Inactive Publication Date: 2020-04-28
GUILIN UNIVERSITY OF TECHNOLOGY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

About 10.1 million people around the world suffer from malignant tumors every year. The discovery of metal anti-tumor drugs such as cisplatin has brought new hope to the treatment of malignant tumors. They have significant curative effects on malignant tumors such as ovarian cancer, bladder cancer, and testicular cancer. However, most metal antineoplastic drugs used clinically have relatively large toxic and side effects, such as liver toxicity, gastrointestinal toxicity, bone marrow toxicity, ototoxicity, neurotoxicity, and nephrotoxicity, which greatly limit their clinical application. usage of

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  • Synthesis method and application of ruthenium (II) polypyridine metal complex with anti-tumor effect
  • Synthesis method and application of ruthenium (II) polypyridine metal complex with anti-tumor effect
  • Synthesis method and application of ruthenium (II) polypyridine metal complex with anti-tumor effect

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Effect test

Embodiment 1

[0028] (1) Take a sealed tube of 25mL, add 1mmol of 4-bromobenzaldehyde, 1.3mmol of 2-ethynylthiophene, 0.1mmol of cuprous iodide, Pd(PPh 3 ) 2 Cl 2 0.05mmol and triethylamine 8mL toluene, under argon protection, stirred at 40°C for 8 hours (the extent of the reaction was detected by TLC), after the reaction was completed, cooled to room temperature and filtered, collected the filtrate, distilled under reduced pressure to remove triethylamine, passed through the column Purified by chromatography to obtain 4-(thiophene-2-ethynyl)benzaldehyde. The eluents used were petroleum ether and ethyl acetate, the volume ratio of which was petroleum ether:ethyl acetate=15:1, and the yield was 75%.

[0029] (2) Take a 150mL three-necked flask, add 1 mmol of 4-(thiophene-2-ethynyl)benzaldehyde, 1 mmol of o-phenanthroline-5,6-dione, 15 mmol of ammonium acetate and 30 mL of acetic acid in sequence, and stir the reaction at 130°C After 4 hours, cool to room temperature after the reaction, a...

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Abstract

The invention discloses a synthesis method and application of a ruthenium (II) polypyridine metal complex. According to the ruthenium (II) complex, 2-(4-(thiophene-2-ethynyl) phenyl)-1H-imidazo [4, 5-f] [1, 10] phenanthroline is used as a main ligand, and 4, 4 '-dimethyl-2, 2'-dipyridyl is used as an auxiliary ligand. The synthesized complex can effectively inhibit proliferation of various tumor cells (A549, HepG-2, SGC-7901 and Hela), in addition, the ruthenium metal complex can effectively inhibit migration of the tumor cells, the content of active oxygen in the cells is remarkably increased, and the ruthenium metal complex is expected to be developed into a medicine for treating various tumors.

Description

technical field [0001] The invention belongs to the field of antitumor drugs, in particular to a ruthenium (II) polypyridine metal complex [Ru(dmb) 2 (ETPIP)] 2+ synthetic methods and applications. Background technique [0002] At present, malignant tumor is one of the main diseases that endanger human health, and the patients who died of cancer accounted for about 25% of the total disease deaths. About 10.1 million people around the world suffer from malignant tumors every year. The discovery of metal anti-tumor drugs such as cisplatin has brought new hope to the treatment of malignant tumors. They have significant curative effects on malignant tumors such as ovarian cancer, bladder cancer, and testicular cancer. However, most of the metal antineoplastic drugs used clinically have relatively large toxic and side effects, such as hepatotoxicity, gastrointestinal toxicity, bone marrow toxicity, ototoxicity, neurotoxicity and nephrotoxicity, which greatly limit their clinica...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61P35/00
CPCC07F15/0053A61P35/00
Inventor 蒋光彬王守才及方华
Owner GUILIN UNIVERSITY OF TECHNOLOGY
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