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acylhydrazone Schiff base platinum complex and synthesis method and application thereof

An acylhydrazone Schiff base platinum, synthesis method technology, applied in the field of platinum complexes, can solve problems such as limited clinical application, achieve significant cell proliferation, good in vitro tumor growth inhibition activity, and cell proliferation inhibition effects

Inactive Publication Date: 2018-12-18
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Platinum drugs are new inorganic anti-tumor drugs developed in the 1960s. After decades of research and development, cisplatin, carboplatin, oxaliplatin, and nedaplatin have been successfully developed for global use. Clinical drugs, these compounds have played an important role in the treatment of malignant tumors, especially cisplatin and carboplatin are currently one of the most widely used anti-tumor drugs in clinical practice, and are the first choice for the treatment of many tumors. Severe adverse reactions in normal tissues often limit its clinical application. For example, the adverse reactions of cisplatin include ototoxicity, gastrointestinal toxicity, bone marrow suppression and renal toxicity. The relentless pursuit of scientific researchers from all over the world

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  • acylhydrazone Schiff base platinum complex and synthesis method and application thereof
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  • acylhydrazone Schiff base platinum complex and synthesis method and application thereof

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Embodiment 1

[0021] Embodiment 1. The preparation of acylhydrazone Schiff base platinum complex of the present invention in methanol

[0022] Weigh HPEBH (0.3mmol, 0.0768g) into a round bottom flask, add 30ml of methanol, stir the solution with slight heat to dissolve, wait until it is completely dissolved, cool at room temperature, then add K dissolved in 2ml of water dropwise 2 PtCl 4 (0.3mmol, 0.125g) solution, under nitrogen protection, heated and stirred, refluxed at 80°C for 5h, a light brown solid powder was precipitated, and the product was filtered after the reaction was complete. The solid powder was washed three times successively with water, methanol and diethyl ether, and dried in vacuum to obtain 0.1069 g of light brown solid powder with a yield of about 73%. Elemental analysis results press C 13 h 11 ClN 4 o 2 Pt(2) calculation. Theoretical (%): C 32.14, H 2.28, N 11.53; Experimental (%): C 32.33, H 2.69, N 11.89. The obtained light brown solid powder was dissolved in...

Embodiment 2

[0023] Embodiment 2. The preparation of the acylhydrazone Schiff base platinum complex of the present invention in ethanol

[0024] Weigh HPEBH (0.3mmol, 0.0768g) into a round bottom flask, add 40ml of ethanol, stir and dissolve the solution with slight heat, cool at room temperature after it is completely dissolved, then add K dissolved in 2ml of water dropwise 2 PtCl 4 (0.3mmol, 0.125g) solution, under nitrogen protection, heated and stirred, refluxed at 70°C for 5h, a light brown solid powder was precipitated, and the product was filtered after the reaction was complete. The solid powder was washed three times successively with water, ethanol and ether, and dried in vacuum to obtain 0.0986 g of light brown solid powder, with a yield of about 68%. The obtained light brown solid powder was dissolved in dimethyl sulfoxide to form a supersaturated solution, filtered, and the filtrate was collected into a special small test tube for diffusion, and acetonitrile was used as a dif...

Embodiment 3

[0025] Example 3. Experimental Conditions and Results of Acylhydrazone Schiff Base Platinum Complex Single Crystal X-ray Diffraction of the Present Invention

[0026] The test was carried out at the Beijing Synchrotron Radiation (BSRF) 3W1A line station. The test is carried out with a Bruker APEX-II CCD diffractometer, with graphite monochromator Mo-Kɑ as the radiation source, at a wavelength of under conditions. Collect the X-ray diffraction data of the corresponding single crystal, use the SMART software to determine the unit cell parameters, and use the SAINTPlus program to restore and correct the data. The initial structure was resolved using the SHELXS97 (Sheldrick, 2008) package, and then refined using the SHELXL97 (Sheldrick, 2008) package. The crystal structure of the complex is attached figure 1 , and some other details about the crystals are listed in Table 1.

[0027] Table 1 Crystallographic data of acylhydrazone Schiff base platinum complexes

[0028]

[...

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Abstract

The invention provides an acylhydrazone Schiff base platinum complex and a synthesis method and application thereof. The comple has the formula of C13H11ClN4O2Pt(1), wherein a ligand is 2-hydroxy-N'-(1-(pyrazine-2-yl)ethylidene) benzoyl hydrazone (HPEBH). The synthesis method of the complex is as follows: dissolving the ligand HPEBH in methanol or ethanol, dropwise adding a K2PtCl4 aqueous solution, introducing nitrogen gas, heating and stirring, heating for refluxing for 4 to 8 hours to precipitate a light brown solid, filtering, washing, drying under vacuum, dissolving dried solid powder ina polar solvent, and using an acetonitrile diffusion method to obtain a brown transparent block crystal with the yield of 40-75%. Experimental studies on proliferation inhibition of tumor cells and normal cells in vitro show that the complex has a good inhibitory effect on the proliferation of human hepatoma cell HepG2, but is not obvious in effect on the proliferation inhibition of normal mouse macrophage Raw246.7, and compared with cis-platinum, the complex has better antitumor activity and lower toxicity.

Description

technical field [0001] The invention relates to the field of platinum complexes and the technical field of chemically synthesized drugs, in particular to an acylhydrazone Schiff base platinum complex and a synthesis method thereof, as well as the application of the complex in the synthesis of antitumor drugs. Background technique [0002] Malignant tumors have been regarded as an invincible fortress for many years, and they are one of the most important diseases that threaten human life. In order to deal with this "killer of life", researchers from all over the world have been working unremittingly in various fields, hoping that with the development of science and technology and the deepening of human understanding of themselves and the world, people can cure this disease as soon as possible. At present, the treatment methods for malignant tumors mainly include chemical drug therapy, radiotherapy, and surgical treatment, among which chemical drugs (especially platinum drugs)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0093
Inventor 袁彩霞王矗王建薇卢丽萍朱苗力
Owner SHANXI UNIV