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Golden phosphorous acetyletic compound, and preparation method and applications thereof

A compound, gold phosphoryne technology, applied in the field of new gold phosphoryne compounds, can solve the problem of loss of biological activity, and achieve the effect of good tumor inhibition, wide application prospect and strong stability

Active Publication Date: 2013-12-25
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented new type of chemical called Phosphorus (P) describes an organism that produces special substances like pigment or other small molecules made from certain proteins found inside cells. These tiny particles are harmful if they get into our bloodstream causing damage when infected by bacteria such as Escherichia coli. People have been trying for years to find ways to prevent these harm caused by this process.

Problems solved by technology

The technical problem addressed in this patents relates to finding novel stable metallothene antibodies from natural sources which could potentially provide effective therapy against various types of solid malignancy disease like leukemia.

Method used

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  • Golden phosphorous acetyletic compound, and preparation method and applications thereof
  • Golden phosphorous acetyletic compound, and preparation method and applications thereof
  • Golden phosphorous acetyletic compound, and preparation method and applications thereof

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Experimental program
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Effect test

Embodiment 1

[0042] Embodiment 1 The preparation of the gold phosphyne compound of the present invention (the R structure is p-methoxyphenyl, and the R' structure is 2-thiophene diphenylphosphine)

[0043] Add chloroauric acid (800mg, 1.94mmol), 1.12g potassium bromide, 4mL water into a 50mL two-necked flask, stir to dissolve it, add 14mL of acetone-water (1:1) solution, the solution of the reaction system is dark red. In an ice bath, sulfur dioxide was slowly introduced until the color of the reaction system turned light yellow.

[0044] Add 0.8mL of acetone solution dissolved with p-methoxyphenyl alkyne (2.04mmol), 1.6g of sodium acetate, and then react at room temperature for 1h. A large amount of yellow solids are formed. After the reaction is completed, filter with suction, and filter the cake with acetone and Wash with ether.

[0045] Add 0.1mmol of the gold alkyne compound prepared above, 0.1mmol of 2-thiophene diphenylphosphine ligand, and 2ml of dichloromethane into a 15mL press...

Embodiment 2

[0050] Embodiment 2 The preparation of the aurophosphyne compound of the present invention (the R structure is phenyl, and the R' structure is 2-thiophene diphenylphosphine)

[0051] Add chloroauric acid (800mg, 1.94mmol), 1.12g potassium bromide, 4mL water into a 50mL two-necked bottle, stir to dissolve, add 14mL of acetone-water (1:1) solution, the solution of the reaction system is dark red. In an ice bath, sulfur dioxide was slowly introduced until the color of the reaction system turned light yellow.

[0052] Add 0.8mL of acetone solution dissolved in phenylyne (2.04mmol), 1.6g of sodium acetate, and then react at room temperature for 1h, a large amount of yellow solid is formed, after the reaction is completed, filter with suction, and wash the filter cake with acetone and ether respectively.

[0053] Add 0.1mmol of the gold alkyne compound prepared above, 0.1mmol of 2-thiophene diphenylphosphine ligand, and 2ml of dichloromethane into a 15mL pressure-resistant tube, re...

Embodiment 3

[0058] The stability test of embodiment 3 gold phosphyne compound of the present invention

[0059] The stability test program is as follows:

[0060] Dissolve 6 mg of bovine serum albumin (BSA) in 0.6 mL of water as a stock solution. Add 20 μM of the auropharyne compound prepared in Example 1 and Example 2 and the other three as controls to the 10-fold diluted BSA solution, take 2 μL of the solution every 30 minutes, and use matrix-assisted laser desorption ionization time-of-flight mass spectrometry to test The molecular weight of BSA protein changes with time; the stability of the compound is verified by the strength of the ligand exchange between the gold phosphyne compound and BSA. The result is as figure 2 , image 3 shown.

[0061] figure 2 The results show that: a is the aureophosphyne compound prepared in Example 1, and b, c, and d are three kinds of aureophosphyne compounds used as controls. Compared with b, c, and d reference compounds, the BSA molecular wei...

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Abstract

The invention discloses a golden phosphorous acetyletic compound in the general formula, and a preparation method and applications thereof. The golden phosphorous acetyletic compound has stronger in-vivo stability, and can efficiently and specifically inhibit the activity of thioredoxin reductase in a targeted manner, thus inhibiting the increase of tumor through damaging intracellular redox level; in addition, better in-vitro and in-vivo tumor inhibition effects can be achieved, the targeted tumor treatment effect can be realized, and the golden phosphorous acetyletic compound has wide application prospects.

Description

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Claims

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Application Information

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Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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