Application of 5-substituted-2,4-thiazolidinedione compound in preparation of IGF1R (insulin-like growth factor 1 receptor) function regulating medicaments

A technology of thiazolidinediones and compounds, applied in the fields of medicinal chemistry and pharmacotherapy

Inactive Publication Date: 2011-06-01
EAST CHINA UNIV OF SCI & TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The novel 5-substituted-2,4-thiazolidinedione compound we discovered has the activity of inhibiting the catalytic action of the IGF1R kinase domain, and there has never been any relevant report on the use of the compound of the present invention in the preparation of drugs for cancer-related diseases

Method used

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  • Application of 5-substituted-2,4-thiazolidinedione compound in preparation of IGF1R (insulin-like growth factor 1 receptor) function regulating medicaments
  • Application of 5-substituted-2,4-thiazolidinedione compound in preparation of IGF1R (insulin-like growth factor 1 receptor) function regulating medicaments
  • Application of 5-substituted-2,4-thiazolidinedione compound in preparation of IGF1R (insulin-like growth factor 1 receptor) function regulating medicaments

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] The compound provided by the invention is obtained through virtual screening by computer-aided drug design method.

[0045] The present invention comprehensively uses structure-based pharmacophore matching and receptor-based molecular docking methods to perform virtual screening on the SPECS compound database (230,000 chemical molecular structures) of the Dutch SPECS Chemical Company, and finally obtains the compound provided by the present invention through screening Specific examples 1 to 75 of .

[0046] (1) The structure-based pharmacophore matching method was used to screen the SPECS database.

[0047] Starting from the complex crystal structure of IGF1R and its small molecule inhibitor BMI (PDB database number 2OJ9), LigandScout was used to generate a pharmacophore model capable of characterizing the interaction mode of IGF1R and BMI. Using this model as a questioning model, the pharmacophore module in DiscoverySturdio 2.0 was used to match the three-dimensional ...

Embodiment 2

[0051] In vitro inhibitory effect of compounds provided by the invention on insulin-like growth factor 1 receptor (IGF1R) kinase activity

[0052] Material:

[0053] The tyrosine kinase used in the experiment is obtained by expressing and purifying the insect baculovirus expression system. Poly (Glu, Tyr) 4:1 It is the product of Sigma Company (St Louis, MO, USA); ATP and OPD are the products of Amresco Company (Solon, Ohio, USA); the anti-phosphotyrosine monoclonal antibody PY99 is the product of Santa Cruz Company (Santa Cruz, CA, USA) products; horseradish peroxidase-labeled goat anti-mouse IgG is a product of Calbiochem (Darmstadt, Germany); the microtiter plate is a product of Corning (New York, USA).

[0054] method:

[0055] The biological activity test method is a tyrosine kinase activity test based on enzyme-linked immunofluorescence analysis.

[0056] (1) Use 20g / ml concentration of enzyme reaction substrate Poly(Glu, Tyr) 4:1 Pre-coated microtiter plates;

[0...

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Abstract

The invention relates to an application of a 5-substituted-2,4-thiazolidinedione compound as shown in general formula (I) disclosed in the specification or pharmaceutically acceptable salts thereof in the preparation of IGF1R (insulin-like growth factor 1 receptor) function regulating medicaments. The 5-substituted-2,4-thiazolidinedione compound has a better effect in the aspect of inhibiting IGF1R kinase activity, and the IGF1R plays an important role in promoting the proliferation and differentiation of tumor cells, so that the compound provided by the invention can be used for preparing the medicaments for treating tumor diseases.

Description

technical field [0001] The present invention relates to the fields of medicinal chemistry and pharmacotherapeutics. Specifically, the present invention relates to the application of 5-substituted-2,4-thiazolidinedione compounds in the preparation of medicines for treating cancer-related diseases. The internal tyrosine kinase activity has the potential use of treating tumor or cancer diseases. Background technique [0002] Cancer is a chronic disease that seriously endangers human health. There are 9 million people suffering from cancer in the world every year, and 6 million patients who die from cancer. In my country, the annual incidence of cancer is about 1.2 million, and the number of people who die from cancer every year is as high as 900,000, and more than 1.5 million patients are waiting for treatment. Overcoming the difficulty of cancer is a major task for medical workers. [0003] The drugs that have been studied and applied by people for a long time regard cancer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61K31/427A61K31/4439A61K31/5377A61K31/428A61K31/4709A61P35/00
CPCA61K31/426A61K31/427A61P35/00
Inventor 蒋华良丁健李洪林谢华刘晓峰童林江徐玉芳
Owner EAST CHINA UNIV OF SCI & TECH
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