Ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity as well as preparation method of complex and protein tyrosine phosphatase 1B inhibitor

A technology of tyrosine phosphatase and ruthenium complexes, which can be applied to compounds containing elements of Group 8/9/10/18 of the periodic table, chemical instruments and methods, drug combinations, etc., can solve the problem of hindering lung metastasis and delaying tumors development process and other issues to achieve a good inhibitory effect

Inactive Publication Date: 2013-10-23
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Loss of PTP1B delays tumor progression and impedes lung metastases in a c-erbB2-induced mouse breast cancer model

Method used

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  • Ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity as well as preparation method of complex and protein tyrosine phosphatase 1B inhibitor
  • Ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity as well as preparation method of complex and protein tyrosine phosphatase 1B inhibitor
  • Ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity as well as preparation method of complex and protein tyrosine phosphatase 1B inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] This example is used to illustrate the preparation of the ruthenium-containing complex for inhibiting the activity of protein tyrosine phosphatase 1B of the present invention.

[0044]

[0045] (1) In the mixed solution of liquid ammonia and ethanol, at -78°C, mix the aromatic hydrocarbon with metal sodium for 1 hour (the molar ratio of liquid ammonia, ethanol, aromatic hydrocarbon and sodium is 250:10:1:5), to obtain Dihydrogenated aromatic hydrocarbons; the aromatic hydrocarbons are p-methylcymene; then the reaction product is subjected to vacuum distillation at 50-150°C to remove the solvent and some unreacted raw materials, and it is obtained by nuclear magnetic resonance analysis. In the reaction product mixture , the purity of dihydroaromatics is about 70% by weight;

[0046] (2) The reaction product mixture containing dihydroaromatics and ruthenium chloride are contacted in ethanol, wherein, the consumption of the reaction product mixture containing dihydroaro...

Embodiment 2

[0052] This example is used to illustrate the inhibitory activity of ruthenium-containing complexes on protein tyrosine phosphatase 1B (PTP1B).

[0053] In this example, dithiothreitol (DTT) was purchased from Pierce Company, MOPS was purchased from AMRESCO Company, pNPP was purchased from Alfa Company, and NaOH was purchased from Beijing Chemical Reagent Company, all of which were of analytical grade.

[0054] First, 10 μL of ruthenium compounds with different concentrations (200 μM, 100 μM, 10 μM, 1 μM, 0.1 μM and 0.01 μM, respectively, 6 samples for each concentration) were added to 70 μL of 20 mM MOPS buffer, and PTP1B was added, and the amount of PTP1B added was such that The final concentration of PTP1B in the mixture was 250nM. After the mixture was incubated at 25°C for 30min, 5 μL of DTT (DTT concentration was 2mM) was added, and incubated at the same temperature for another 30min to maintain the activity of the enzyme. Then 10 uL of pNPP (0.02M) substrate was added. ...

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Abstract

The invention discloses a ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity and a preparation method of the complex. The invention further discloses a protein tyrosine phosphatase 1B inhibitor which contains the ruthenium-containing complex. The ruthenium-containing complex for inhibiting protein tyrosine phosphatase 1B activity disclosed by the invention is a complex as shown in formula (1), wherein in the formula (1), A is one of structures as shown in formulas (2)-(8), and X is halogen. The ruthenium-containing complex has good protein tyrosine phosphatase 1B inhibiting activity.

Description

technical field [0001] The invention relates to a ruthenium-containing complex for inhibiting the activity of protein tyrosine phosphatase 1B, a preparation method thereof and a protein tyrosine phosphatase 1B inhibitor. Background technique [0002] The phosphorylation level of intracellular tyrosine plays an important role in the process of intracellular signal transduction. It is related to the growth, differentiation, metabolism, cell migration and gene transcription, ion channel activity, immune response, apoptosis, etc. of cells in vivo. process are closely related. Protein tyrosine phosphatase 1B (protein tyrosine phosphatase, PTP1B) is a classic non-receptor tyrosine phosphatase in the protein tyrosine phosphatase (protein tyrosine phosphatases, PTPs) family, which was first purified and identified Biological characterization of protein tyrosine phosphatases. Changes in PTP1B expression are associated with a variety of human diseases, including obesity, type 2 diab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P3/04A61P3/10A61P35/00
Inventor 汪福意韩玉苗罗群郑伟吴魁李鲜婵
Owner INST OF CHEM CHINESE ACAD OF SCI
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