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Selenium thioxo cysteine benzamide compound and preparation method and application thereof

A technology of cystine benzamide and cysteine, which is applied in the directions of active ingredients of heterocyclic compounds, organic chemistry, drug combination, etc., can solve the problems of poor solubility of organic selenium compounds, limited medical use and application scope, etc. , to achieve the effect of good water solubility, stable properties and stable aqueous solution

Inactive Publication Date: 2010-07-28
曾慧慧
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These applications or patents all disclose 2-phenyl-1,2-benzisoselazol-3(2)-ketones having antitumor activity, immunomodulatory and biotherapeutic activity, antifibrosis and inhibition of gelatinase activity. (hereinafter referred to as "ethaneselenium") and its derivatives, but the solubility of these organic selenium compounds is not good, which limits its medical use and application range

Method used

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  • Selenium thioxo cysteine benzamide compound and preparation method and application thereof
  • Selenium thioxo cysteine benzamide compound and preparation method and application thereof
  • Selenium thioxo cysteine benzamide compound and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0049] Example 1 Preparation of 1,2[bis(2-selenothiocysteine ​​benzamide)]ethane

[0050] 1) Wet 100mg of ethaneselenoline with 10ml of ethanol and disperse ultrasonically;

[0051] 2) Dissolve 0.28g-cysteine ​​in 5ml water;

[0052] 3) Under stirring conditions, add the ethyl selenoline ethanol solution obtained in step 1) to the L-cysteine ​​obtained in step 2), mix well, and adjust the pH value to alkaline with 1M aqueous sodium hydroxide to make Completely dissolve, freeze-dry or rotary evaporate, dry, and get ready.

[0053] The resulting 1, 2 [bis(2-selenomercaptocysteine ​​benzamide)] ethane (hereinafter referred to as "ethane selenoline / CYS") aqueous solution has a pH between 7.5 and 12, and the lyophilized product is used The physiological saline dissolves, shows good reconstitution, and the prepared intravenous injection has good stability.

[0054] The ESI mass spectrum of ethaneselenoline / CYS shows that the molar ratio of ethaneselenoline to cysteine ​​compound is 1:2 (MW...

Embodiment 2

[0056] Example 2 Ethylselenoline / CYS inhibits the growth of tumor cells in mice

[0057] 2.1 Experimental method

[0058] 84 Kunming male mice weighing 20±2g, H22 liver cancer cells were diluted with saline at a ratio of 1:3 to obtain a liver cancer cell suspension. The liver cancer cell suspension was injected subcutaneously into the right forelimb axilla of the mouse. After 0.2ml of liquid, they were randomly divided into 7 groups, including ethaneselenoline / CYS intravenous injection group, ethaneselenoline / CYS intraperitoneal injection group, oral ethaneselenoline / CYS high-dose group, oral instillation of ethaneselenoline / CYS group, oral ethane selenoline / CYS low dose group, oral ethane selenoline suspension group and normal saline group. Since 24h after vaccination, the drug will be administered according to body weight.

[0059] 2.2 The mode of administration and dosage of each group in the experiment

[0060] Ethylselenoline / CYS intravenous injection group: Weigh 78.925mg e...

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Abstract

The invention discloses a selenium thioxo cysteine benzamide compound and a pharmaceutically acceptable salt thereof. Compared with the dissolvability of ethaselen and derivatives thereof, the dissolvability of the selenium thioxo cysteine benzamide compound is improved, thus the selenium thioxo cysteine benzamide compound has excellent anti-tumor effect and more wide medicinal application.

Description

Technical field [0001] The invention relates to a new type of organic selenium compound, in particular to selenomercaptocysteine ​​benzamide compounds and a preparation method and application thereof. Background technique [0002] CN1166651C, CN1281593C, CN1242999C, CN1280279A, CN1704408A, CN1704409A, CN1704410A, CN1853627A and CN1990475A respectively disclose "R-double or glycobenzyl isoselenazole substituted compounds with anti-inflammatory and anti-tumor effects" and "benziisoselazole derivatives" "Immune regulation and biotherapeutic effects of selenium", "Benzisoselazole derivatives and their applications", "Dibenzis isoxazolones and their synthesis and applications", "Isselazolones and their complexes and "Applications", "Compounds with anti-fibrosis and gelatinase activity inhibition and their applications", "Benzisoselazolone derivatives and their preparation methods and applications", "Dibenzisoselazolidine cyclodextrin Or cyclodextrin derivative inclusion compound and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C391/02C07D293/10A61K31/095A61K31/41A61P35/00A61P35/02
Inventor 曾慧慧崔翰明
Owner 曾慧慧