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A kind of hexavanadate-beta-alanine tert-butyl ester derivative and its preparation method and application

A technology of tert-butyl alanine and succinic acid hexavanadate, which is applied in the field of tert-butyl hexavanadate-β-alanine tert-butyl ester derivatives and its preparation, can solve the problem of prolonging the survival time of cancer patients who cannot be completely cured Cancer and other problems, to achieve the effect of easy mass production and promotion, great research value and application prospect, and low cost

Active Publication Date: 2020-03-10
HUBEI UNIV OF TECH
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Problems solved by technology

With the advancement of society's science and technology, human beings' understanding of cancer has gradually become clearer, and the methods, technologies and theories for the prevention and early diagnosis of certain cancers have also become more mature, but they cannot completely cure cancer, and can only prolong the life of cancer in a very limited way. patient survival time

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  • A kind of hexavanadate-beta-alanine tert-butyl ester derivative and its preparation method and application
  • A kind of hexavanadate-beta-alanine tert-butyl ester derivative and its preparation method and application
  • A kind of hexavanadate-beta-alanine tert-butyl ester derivative and its preparation method and application

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Embodiment 1 6

[0024] The synthesis of embodiment 1 hexavanadic acid-beta-alanine tert-butyl ester derivatives

[0025] The anion structure of hexavanadate-β-alanine tert-butyl ester derivative is as follows figure 1 As shown, it is Linqivist-type hexavanadate, in which all the vanadium is +5, and the oxygen atom on the hexavanadate is replaced by the hydroxyl oxygen of two trimethylol compounds, and each trimethylol The three hydroxyl oxygens on the compound replace the three bridging oxygen atoms arranged in a planar triangle on the hexavanadate, and the two trimethylol compounds are relatively distributed on the hexavanadate skeleton. The compounds are covalently linked.

[0026] The synthesis of hexavanadate-β-alanine tert-butyl ester derivatives is carried out in three steps, and the schematic diagram of the synthesis process is as follows: figure 2 shown.

[0027] (1)[Bu 4 N] 2 [V 6 o 13 {(OCH 2 ) 3 CCH 2 OH} 2 ] Synthesis of Pentaerythritol Hexavanadate Derivatives

[002...

Embodiment 2

[0034] Embodiment 2 antitumor activity evaluation

[0035] (1) In vitro antitumor activity evaluation of compounds

[0036] Tested tumor cells: human liver cancer cell HepG2, human rhabdomyoma cell RD, human cervical cancer cell Hela, human laryngeal cancer cell Hep-2, human breast cancer cell MCF-7.

[0037] Cell culture: GIBCO DMEM medium, 10% fetal bovine serum and 0.01% L-glutamine were prepared as culture medium. Cultured cell lines were placed at 37°C, 5% CO 2 The cells were routinely cultured and subcultured under saturated humidity, and the cells in the logarithmic growth phase were used in the experiments.

[0038] In vitro anti-tumor activity evaluation (MTT method): the above tumor cells were respectively plated in 96-well plates, and at 37°C, 5% CO 2 After the incubator was cultured to cover the monolayer, the cell culture medium was discarded, and the cell maintenance solution (containing serum 2% and 0.002% L-glutamine) containing different concentrations of t...

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Abstract

The invention discloses a hexa-vanadic acid-beta-alanine tert-butyl ester derivative and a preparation method and application thereof and belongs to the technical field of organic and inorganic hybridmaterials. The hexa-vanadic acid-beta-alanine tert-butyl ester derivative has antineoplastic activity, and a structural formula of the derivative is [Bu4N]2[V6O13 {(OCH2)3 CCH2OOCCH2CH2CONHCH2CH2COOC(CH3)3 } 2]. The preparation method of the derivative includes the following steps that 1-(3-dimethylamino propyl)-3-ethyl carbodiimide hydrochloride, 1-phenolan benzotriazole, beta-alanine tert-butylester hydrochloride and triethylamine are added into an acetonitrile solution of a hexa-vanadic acid-succinic acid derivative, and after the mixture above is completely dissolved, the mixture is subjected to a reaction at 48-52 DEG C for 40-50 hours to obtain the hexa-vanadic acid-beta-alanine tert-butyl ester derivative. The hexa-vanadic acid-beta-alanine tert-butyl ester derivative has a significant research value and a great application prospect in the medicinal chemistry field and provides a direction for further development of medicine.

Description

technical field [0001] The invention relates to the technical field of organic-inorganic hybrid materials, in particular to a derivative of tert-butyl hexavanadic acid-β-alanine and its preparation method and application. Background technique [0002] Malignant tumor is a common and frequently-occurring disease that seriously threatens human health. The mortality rate of human beings caused by malignant tumors ranks second among all diseases, becoming the second "killer" after cardiovascular diseases. At the beginning of 2013, the National Cancer Registry Center issued a version of the "2012 China Cancer Registration Annual Report", indicating that there are about 3.12 million new cancer cases in China every year, and more than 2 million cancer deaths, which means that 6 people are diagnosed with cancer every minute. cancer. At present, the incidence of cancer in the whole country is severe, and the incidence and mortality are on the rise. Cancer has become one of the majo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/00A61K31/28A61P35/00
CPCA61P35/00C07F9/005
Inventor 伍平凡熊哲伦肖滋成
Owner HUBEI UNIV OF TECH
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