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Water-soluble derivative of diphenylethene compounds, preparation method and usage thereof

A stilbene-based, water-soluble technology, applied in chemical instruments and methods, compounds of Group 5/15 elements of the periodic table, medical preparations containing active ingredients, etc., can solve problems such as increased cost and weak water solubility , to achieve the effect of low cost, high efficiency, simple and reliable preparation method

Inactive Publication Date: 2012-10-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Some studies have isolated the compound trans-4-[2- (3,5-dimethoxyphenyl)vinyl]-1,2-benzenediol, as shown by tests, has obvious anti-tumor effect (ZL 200710041994.1, ZL200710041995.6); however, practice shows that, Due to the relatively weak water solubility of this compound, it is limited by the characteristics of the compound itself, which obviously increases the cost in drug development and application. applications in the field

Method used

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  • Water-soluble derivative of diphenylethene compounds, preparation method and usage thereof
  • Water-soluble derivative of diphenylethene compounds, preparation method and usage thereof
  • Water-soluble derivative of diphenylethene compounds, preparation method and usage thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Preparation of Trans-4- [2- (3,5-dimethyl oxygenyl) ethylene group] -1, 2-benzhenyl phosphate di sodium salt

[0039] (O-Shu Ding) -TRANS-4- [2- (3, 5-dimer oxygenyl) ethylene group] -1, 2-benzhenol phosphate 10 g, methanol 100 ml add 500 ml to 500 mLIn the reaction bottle, the dry hydrogen chloride gas is applied in an appropriate amount, the temperature is increased to 40-50 degrees for 24 hours, filtering, decompression to remove solvents, the product is consolidated with acetone, the phosphate of the compound, filtering, drying, and 2 m NaOH of 2 m NaOHIn the methanol, the salt, filtering, adding acetone to analyze white solids, and 6.1 grams of dry products.The compound of the income compound performed a nuclear magnetic resonance analysis, and the results were shown in Table 1.

[0040] Table 1 TRANS-4- [2- (3,5-dimer oxygenyl) ethylene groups] -1, 2-benzhenyl phosphate di-sodium salt duty magnetic resonance data

[0041] (( 1 H nmr 500 mHz, 13 C NMR 500 MHz in CDCL ...

Embodiment 2

[0043] Example 2 Trans-4- [2- (3, 5-dimer oxygenyl) ethylene groups] -1, 2-phenyl alcohol phosphate sodium saline test

[0044] Take the correct number of cells 3 × 10 per hole 4 After inoculation on the 96 -hole board, after 12 hours, abandon the Qing Dynasty, and click the group to administer: the normal control group and the addition of the medicine group (concentration 0-100 μm), each group is set 6 to cultivate 24h, abandon the Qingqing, discard the Qing Dynasty, discard the clearing, and abandon the Qing Dynasty.Add 50 μl of medium with MTT to cultivate 4H (0.5 mg / ml), add 100 μL DMSO, oscillate 1h, and test the OD value at 570 nm on the enzyme marker.

[0045]The results showed that after adding medicine, cell activity decreased significantly, and cell activity decreased with the increase of drug concentration.For SF188 (cerebral gel tumor cells), HGC-27 (gastric cancer cells), MCF-7WT (breast cancer cells), H460 (large cell lung cancer cells) (cell strains are purchased fr...

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Abstract

The invention belongs to the field of antineoplastic compounds and relates to a water-soluble derivative of diphenylethene compounds, especially a water-soluble derivative of trans-4-[2-(3,5-dimethoxyphenyl)vinyl]-1,2-benzenediol as shown in the formula I, a preparation method and a usage thereof in the preparation of antitumor drugs. The water-soluble derivative of diphenylethene compounds is prepared through water-soluble reconstruction by taking the compound, trans-4-[2-(3,5- dimethoxyphenyl)vinyl]-1,2-benzenediol, as a parent nucleus. Results of in vitro antineoplastic tests show that the water-soluble derivative of diphenylethene compounds has significant effects in inhibiting brain glioma cells SF188 and U87wt, breast cancer cells MCF-7wt and large cell lung cancer cells H460. The activity of the cells decreases along with the increase of drug concentration. The derivative disclosed by the invention is an effective antitumor agent and further, the derivative can be used for preparing the antitumor drugs.

Description

Technical field [0001] The present invention is a water-soluble derivative of an anti-tumor compound, involving a di-styrene compound, especially the transliteration of antis- [2- (3,5-dimethyl oxygenyl) ethylene groups] -1,2-phenyl-diol water-soluble derivatives and their preparation methods and use in preparation of anti-tumor drugs. Background technique [0002] According to reports, more than 6 million people in the world died of various cancers each year and 8 million new cases. The data is still increasing year by year.There are millions of new cancer patients every year in my country, about 2 million patients to be treated, and more than 1 million deaths. Cancer has become the first cause of death.Therefore, studying the preparation of anti -tumor drugs has become a hot spot in the field of biomedicine. [0003] There are studies from SPHAEROPHYSA SALSULA (Pall.) DC.)-1,2-benzhenyl glycol, which shows that it has obvious anti-tumor effects (ZL 200710041994.1, ZL20071004199...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/12A61K31/6615A61P35/00
Inventor 朱焕章马忠俊
Owner FUDAN UNIV
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