Lindeqvist type tungsten vanadate trimethylolethane derivative as well as preparation method and application thereof

A technology for trimethylolethane tungstate vanadate and derivatives, which is applied in the field of antitumor drug synthesis and achieves the effects of simple preparation method, high yield, mild and controllable reaction conditions

Pending Publication Date: 2021-12-03
HUBEI UNIV OF TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is of great significance and a great challenge to design corresponding new anti-lung cancer drugs with high efficiency and low toxicity.

Method used

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  • Lindeqvist type tungsten vanadate trimethylolethane derivative as well as preparation method and application thereof
  • Lindeqvist type tungsten vanadate trimethylolethane derivative as well as preparation method and application thereof
  • Lindeqvist type tungsten vanadate trimethylolethane derivative as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Synthesis of Lindqvist type tungstovanadate trimethylolethane derivatives

[0029] Lindqvist type tungstovanadate trimethylolethane derivative synthetic process schematic diagram of the present invention is as follows figure 2 Shown, the specific operation steps of synthetic process are as follows:

[0030] Weigh 3.3g sodium tungstate, 1.2g sodium metavanadate, 1.36g trimethylolethane, dissolve in 30ml ultrapure water, then add 1mol / L hydrochloric acid dropwise to the solution to adjust the pH of the solution to 2 -3, react at 85°C for 24h. After the reacted solution was filtered and waited for its natural volatilization, crystals were obtained after about a week, that is, the Lindqvist-type trimethylolethane tungstovanadate derivative described in the present invention.

[0031] Through single crystal X-ray diffraction and XPS detection and analysis, the chemical structural formula of the Lindqvist type trimethylolethane tungstate vanadate derivative is: N...

Embodiment 2

[0032] Example 2 In vitro anti-lung adenocarcinoma A549 cell activity evaluation and normal cytotoxicity evaluation

[0033] This example is used to verify the inhibitory activity of the Lindqvist-type trimethylolethane tungstate vanadate derivative prepared in Example 1 on tumor cells and the low toxicity of normal human cells, as follows:

[0034] (1) Test cells: human lung adenocarcinoma A549 cells, human normal kidney epithelial cells 293T cells.

[0035] (2) Cell culture: GIBCO DMEM medium, culture solution prepared by 10% fetal bovine serum and 0.01% L-glutamine. Cultured cell lines were placed at 37°C, 5% CO 2 Routine culture and subculture at saturation temperature, the experiments were used in the logarithmic growth phase of the cells.

[0036] (3) In vitro anti-tumor activity evaluation (MTT method): the lung adenocarcinoma cell A549 cells were plated on a 96-well plate, and placed at 37 ° C, 5% CO 2After the incubator was cultured to cover the monolayer, the cell...

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Abstract

The invention discloses a Lindeqvist type tungsten vanadate trimethylolethane derivative as well as a preparation method and application of the Lindeqvist type tungsten vanadate trimethylolethane derivative. The structural formula of the Lindeqvist type tungsten vanadate trimethylolethane derivative is Na3 [W2V4O16 (OCH2) 3CCH3]. According to the invention, a compound with excellent anti-tumor activity and obviously reduced killing power to normal cells is obtained by modifying the proportion of organic ligands and parent metal atoms of tungsten vanadate. The Lindeqvist type tungsten vanadate trimethylolethane derivative has the advantages of high stability, good biocompatibility, low toxicity to normal cells, high inhibition rate to adenocarcinoma A549 cells, simple preparation method, mild and controllable reaction conditions, environmental protection, high yield, and extremely high production and application values.

Description

technical field [0001] The invention belongs to the technical field of synthesis of antitumor drugs, and in particular relates to a Lindqvist-type trimethylolethane tungstate vanadate derivative and a preparation method and application thereof. Background technique [0002] Malignant tumors have become a major factor that endangers human life and health. In recent years, due to the gradual increase in the number of smokers in China, as well as the influence of factors such as air pollution and irregular diet, the incidence of lung cancer has not been controlled. According to the global burden of cancer released by the International Agency for Research on Cancer (IARC) under the World Health Organization (WHO), there are approximately 19.3 million new cases and 9.9 million deaths from cancer worldwide. About 37 percent of the cases were from China, and about 39.8 percent of the deaths from lung cancer were from China. This means that about 8 people are diagnosed with cancer...

Claims

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Application Information

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IPC IPC(8): C07F11/00A61P35/00A61K31/28
CPCC07F11/005A61P35/00
Inventor 伍平凡赵晨琪李金成王玉肖滋成
Owner HUBEI UNIV OF TECH
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