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Application of 4-aminopyrimidine compounds

A compound and application technology, applied in the field of Polo-like kinase 1 inhibitor, can solve the problem of not many structural types, and achieve the effect of strong active conformation recognition ability

Inactive Publication Date: 2016-01-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But in general, there are not many PLK1 inhibitors and their structural types at present, and many reported PLK1 inhibitors are non-specific inhibitors, such as Wortmannin, Scytonemin, Staurosporine, morin, ON-01910 and HMN-214, only BI2536, GSK-461364 and LFM-A13 are selective inhibitors of PLK1

Method used

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  • Application of 4-aminopyrimidine compounds
  • Application of 4-aminopyrimidine compounds
  • Application of 4-aminopyrimidine compounds

Examples

Experimental program
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Embodiment 1

[0016] Experimental study on the inhibitory activity of compounds 1 to 4 on PLK1 and tumor cell lines

[0017] 1. PLK1 inhibitory activity test

[0018] 1) Experimental materials: Polo-likekinase Assay / InhibitorScreeningKit, 96-well plate, 10Xwashbuffer, Kinasebuffer, 20XATP, Anti-Phospho-ThreoninePolyclonalPPT-07, HRP-conjugatedAnti-rabbitIgG, SubstrateReagent substrate reagent, StopSolution, PLKpositivecontrol (Cat#CY-E1163Unit concentration per bottle, / 100μL, it needs to be diluted before use to make the concentration 0.1mUnit / well).

[0019] 2) Experimental steps:

[0020] · Solution preparation washbuffer: add 100ml 10Xwashbuffer to 900ml deionized water, mix well. Kinase reaction buffer: add 0.5ml 20XATP to 9.5ml kinase buffer, mix well. Testsample: mother liquor concentration 10 -2 , diluted to 10 with kinasebuffer -5 M for standby. PLKpositivecontrol: Take 1μL PLKpositivecontrol (2Unit / 100μL) and add 1999μL deionized water to prepare a working solution with a ...

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Abstract

The invention relates to the field of medicinal chemistry, in particular to application of 4-aminopyrimidine compounds, 4 compounds (1-4), medical application of medicinal compositions containing the compounds, and especially application of the medicinal compositions serving as Polo-like kinase 1 inhibitors.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to four compounds and pharmaceutical compositions containing these compounds, as well as their medical application, especially the application as Polo-like kinase 1 (PLK1) inhibitor. Background technique [0002] In recent years, tumors have surpassed cardiovascular diseases and become the world's leading cause of death. The research on anti-tumor drugs has important academic and practical significance. [0003] Studies have found that almost all tumors are related to uncontrolled cell growth, blocked differentiation, and abnormal apoptosis caused by the disorder of cell cycle regulation mechanism. The frequency of tumor cell division is faster than that of normal cells, and various proteins that regulate microtubule polymerization, centrosome duplication, spindle formation, and cytokinesis are often overexpressed and their activities are enhanced. An important class of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/505A61K31/506A61P35/00A61P35/02
Inventor 郭晓星
Owner CHINA PHARM UNIV
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