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CDK2 and CSK3beta dual inhibitor and application thereof

A technology of beta inhibitors and uses, applied in the field of medicinal chemistry, can solve the problems of few types of inhibitors and low selectivity of inhibitors

Inactive Publication Date: 2013-12-11
SHANGHAI FOSUN PHARMA DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are fewer types of inhibitors, mainly 3,4-substituted pyrazole derivatives, thiazole derivatives, indazoles and diaminotriazoles, and the relative selectivity of the inhibitors is not high

Method used

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  • CDK2 and CSK3beta dual inhibitor and application thereof
  • CDK2 and CSK3beta dual inhibitor and application thereof
  • CDK2 and CSK3beta dual inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0018] Experimental Study on the Inhibitory Activity of Compound 1~Compound 24 on CDK2 and GSK3β and the Inhibitory Activity on Tumor Cell Lines

[0019] 1. CDk2 inhibitory activity test

[0020] Instrument TECAN Safire 2 Reader (Switzerland Tecan)

[0021] 384-well plate with black wall and bottom (coming company in the United States)

[0022] Plate shaker (Jiangsu Guangming Experimental Instrument Factory)

[0023] Reagent CDK-2 / clyclin A (Invitrogen, USA)

[0024] Z'-LYTE kit 12peptide (Invitrogen, USA)

[0025] DMSO (Sigma, USA)

[0026] [method]

[0027] 1. Add 133 μl of 5× buffer to 367 μl of water to obtain 500 μl of 1.33× kinase buffer.

[0028] 2. Add 0.2 μl CDK-2 / clyclin A and 0.8 μl substrate to 199 μl 1.33× kinase buffer to obtain 200 μl kinase / substrate mixture.

[0029] 3. Add 6 μl of 10 mM ATP to 144 μl of 1.33×kinase buffer to obtain 150 μl of 4×ATP solution.

[0030] 4. Add 0.2 μl of phosphorylated peptide to 49.8 μl of 1.33×kinase buf...

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Abstract

The invention relates to the field of medicinal chemistry, and particularly relates to compounds (1-24) and medical applications of medicinal compositions containing the compounds, especially applications of the medicinal compositions serving CDK2 and CSK3beta dual inhibitors.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to 24 compounds, pharmaceutical compositions containing these compounds and their medical application, especially the application as CDK2 and GSK3β dual inhibitor. Background technique [0002] In recent years, cancer has surpassed cardiovascular disease and become the world's leading cause of death, and the research on anticancer drugs has important academic and practical significance. At present, research focusing on biological targets has become a hot spot in drug development. Relevant studies have shown that the occurrence, development and formation of most diseases are caused by abnormalities in certain proteins. Correcting or regulating abnormal protein functions tends to a normal state. It is possible to achieve the purpose of control or cure. This research and development model has brought great expectations to people, especially for the research and development o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/427C07D233/74A61K31/4166C07D471/10A61K31/438C07D209/38A61K31/404C07D307/42A61K31/341C07C237/22A61K31/198C07D413/14A61K31/506C07D239/36A61K31/513C07D277/46A61K31/426C07C307/06A61K31/18C07D417/06A61K31/454C07D413/06A61K31/5377C07D239/47C07C323/41C07C311/19C07D471/04A61K31/519C07D403/06A61K31/551C07D401/04A61K31/4439A61K31/437C07C317/44A61K31/165A61P35/00
Inventor 陆旖冉挺陆涛王越金建淋袁浩亮
Owner SHANGHAI FOSUN PHARMA DEV CO LTD
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