CDK2 inhibitor and applications thereof

A technology of inhibitors and uses, applied in the field of medicinal chemistry, can solve problems such as inability to phosphorylate substrates, inability to be activated, and loss of kinase activity

Inactive Publication Date: 2016-08-24
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These inhibitors of kinase activity bind Cyclin E-CDK2 to lose kinase activity, unable to phosphorylate its substrate, and DNA synthesis cannot be initiated

Method used

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  • CDK2 inhibitor and applications thereof
  • CDK2 inhibitor and applications thereof
  • CDK2 inhibitor and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Experimental Study on the Inhibitory Activity of Compound 1~Compound 20 on CDK2

[0018] 1. CDK2 inhibitory activity test

[0019] 1) Experimental materials:

[0020] ·CDK2 / cyclin E Kinase

[0021] · Kinase-Glo Plus reagent, including Kinase-Glo Substrate and Kinase-Glo Buffer

[0022] Substrate: Histone H derived peptide: HDB, H09-19T

[0023] Assay Buffer: 25mM HEPES, 10μM MgCl2, 0.01% Triton X-100, 100μm / ml BSA, 2.5mM DTT, pH7.4

[0024] ·ATP

[0025] · White opaque 384-well plate

[0026] 2) Experimental steps:

[0027] · All the compounds to be tested were dissolved in DMSO to prepare a stock solution with a concentration of 100 μM.

[0028] ·Take the compound to be tested and dilute it to 20 μL with assaybuffer to obtain a compound concentration of 10 μM.

[0029] 4*ATP: ATP is diluted with assay buffer to obtain 4*working solution.

[0030] 4*Substrate: The substrate is diluted with assay buffer to obtain 4*working solution.

[0031] ·2.5*CDK2 / cyclin E ...

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Abstract

The invention relates to the field of medicinal chemistry, and in particular to medical applications of compounds (1-20) and medical compositions containing the compounds, especially the applications as the CDK2 inhibitor. The structural formulas of the 20 compounds are shown in the description.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to 20 compounds, pharmaceutical compositions containing these compounds and their medical applications, especially as CDK2 inhibitors. Background technique [0002] Tumor is a common and frequently-occurring disease that seriously endangers human health. In recent years, it has become one of the main causes of human death worldwide. According to the forecast of the World Health Organization, by 2020, the annual number of new cancer patients will reach 15 million. At the same time, the number of cancer deaths is also rising rapidly around the world. In 2007, a total of 7.6 million people died of cancer worldwide. By 2030, the number of cancer deaths may increase to 13.2 million. The task of cancer prevention and treatment is very arduous. [0003] CDK is an important class of serine / threonine protein kinases, which are the engine molecules of cell cycle operation. CDK act...

Claims

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Application Information

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IPC IPC(8): A61K31/454A61P35/00
Inventor 徐金星
Owner CHINA PHARM UNIV
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