Platinum (II) complex, synthetic method and application thereof

A synthetic method and compound technology applied in the field of medicine to achieve good medicinal value and significant anti-tumor activity in vitro

Inactive Publication Date: 2015-07-29
GUANGXI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the study of platinum complexes using 4'-(4-N,N-diethylaminophenyl)-2,2':6',2"-terpyridine as an active ligand is still blank

Method used

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  • Platinum (II) complex, synthetic method and application thereof
  • Platinum (II) complex, synthetic method and application thereof
  • Platinum (II) complex, synthetic method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Accurately weigh 0.5 mmol of ligand L and 0.5 mmol of dichlorobis(dimethylsulfoxide) platinum (II), dissolve ligand L in 35 mL of 85% methanol, and dichloro Two (dimethyl sulfoxide) platinum (II) was dissolved in 20 mL of water, the two solutions were mixed, refluxed at 65 ° C for 36 hours, concentrated and evaporated to remove most of the solvent (75% of the solvent added), cooled After standing at room temperature, the reddish-brown target product was precipitated, and reddish-brown bulk crystals were precipitated after the filtrate was placed for 3 days, and the crystals and powder were collected to obtain the final product (96% yield, the product is the total mass of powder and crystals, the same below).

[0043] The resulting reddish-brown solid product is identified:

[0044] (1) Infrared spectrum:

[0045] IR(KBr):3412,3061,2968,2926,1585,1530,1478,1464,1421,1354,1266,1246,1216,1156,1124,1076,1040,1009,890,818,779,733,716,687,4651,62 -1 .

[0046] (2) Proton N...

Embodiment 2

[0059] Accurately weigh 0.5 mmol of ligand L and 0.5 mmol of dichlorobis(dimethylsulfoxide) platinum (II), and dissolve ligand L in a mixture of 95 mL of 75% methanol and 25% ethanol Solution (the volume ratio of methanol and ethanol is 5:1), dichloro two (dimethyl sulfoxide) platinum (II) is dissolved in the mixed solution of the water of 40mL and 90% methanol (volume of water and methanol ratio of 1:9), the two solutions were mixed, reflux reaction at 85 ° C for 24 hours, concentrated and evaporated to remove most of the solvent (90% of the solvent added), cooled to room temperature and left to stand, and the reddish-brown target product was precipitated. After filtration, reddish-brown crystals were precipitated after standing for 3 days, and the powder and crystals were collected to obtain the final product (yield 75%).

[0060] The resulting final product was analyzed by infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, carbon nuclear magnetic reson...

Embodiment 3

[0062] The amount of accurately weighed substance is 0.5mmol of ligand L and 0.5mmol of dichlorobis(dimethyl sulfoxide) platinum (II), and the ligand L is dissolved in 60mL of dimethyl sulfoxide. Chlorobis(dimethyl sulfoxide) platinum (II) was dissolved in 15 mL of 90% acetone solution, the two solutions were mixed, refluxed at 45°C for 56 hours, concentrated and evaporated to remove most of the solvent (solvent addition amount 82%), cooled to room temperature and stood still, the reddish-brown target product was precipitated, and after filtering, reddish-brown crystals were precipitated after standing for 3 days, and the powder and crystals were collected to obtain the final product (yield 85%).

[0063] The resulting final product was analyzed by infrared spectroscopy, hydrogen nuclear magnetic resonance spectroscopy, carbon nuclear magnetic resonance spectroscopy, electrospray mass spectroscopy and X-ray single crystal diffraction, and was determined to be the target product...

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PUM

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Abstract

The invention discloses a platinum (II) complex, a synthetic method and an application of the platinum (II) complex. The platinum (II) complex takes 4'-(4-N,N-diethylamine phenyl)-2,2':6', 2''-terpyridyl as a ligand. The complex is obtained by dissolving a compound as shown in a formula (II) and dichloro.di(dimethyl sulfoxide)-platinum in a polar solvent and performing a complexing reaction; the complex can be synthesized through a solution method specifically, and can also be synthesized through a solvothermal method. An applicant investigates the proliferating inhibitory activity of the complex to multiple human tumor cell lines, and the results show that the complex has a remarkable antitumor activity in vitro, has good potential medicinal value and is expected to be used for the preparation of all kinds of antitumor drugs. The chemical structural formula of the complex provided by the invention is shown as the following formula (I).

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a platinum (II ) complexes and their synthesis methods and applications. Background technique [0002] As the second leading cause of death among diseases, cancer seriously threatens human health, and its lethal rate accounts for about 25% of the diseases in the world today. In recent years, due to the influence of people's bad living habits and environmental pollution and other factors, the incidence and mortality of cancer have risen sharply, which has become a difficult problem for human beings to overcome. Chemotherapy and radiotherapy are one of the traditional means of treating malignant tumors, and they are widely used clinically and occupy a very important position. Therefore, the research and development of new anticancer drugs is one of the major strategic and hot directions in the field of medicine and health. [0003] Since the 1960s, Rosenberg first discovered th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCC07F15/0093
Inventor 邹华红梁福沛
Owner GUANGXI NORMAL UNIV
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