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Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors

An anti-tumor drug and application technology, applied in the field of anti-tumor pharmacy, can solve problems such as the lack of development of dual-target ERK1 and ERK5 inhibitors, and achieve the effect of inhibiting growth and obvious inhibitory effect

Active Publication Date: 2020-05-12
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Likewise, to date there has been no development of dual-targeted ERK1 and ERK5 inhibitors for the treatment of tumors

Method used

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  • Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors
  • Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors
  • Preparation of dual-targeting ERK1 and ERK5 inhibitor and anti-tumor application of dual-targeting ERK1 and ERK5 inhibitors

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0050] Example 1 Synthesis of preferred compounds.

[0051] Preferred compounds are synthesized using the following reaction formula:

[0052]

[0053] i ethanol, heated to reflux; ii DIEA, acid chloride, room temperature; iii methanol saturated hydrochloric acid solution, 0°C; iv benzyl chloride, K2CO3, DMF, 80°C; v isothiocyanate, DIEA, dichloromethane, room temperature.

[0054] 1. General Synthesis of Intermediates 1-3

[0055]Add tert-butyl 4-opopiperidine-1-carboxylate (30.0mmol), 2-cyanoacetamide (30.0mmol) and sulfur (30.0mmol) in absolute ethanol (200mL) solution, morpholine (30.0 mmol). Stir and reflux for 8 hours, cool the mixture to room temperature, filter, wash with 30ml of ethanol three times, and hang the filtrate to dryness and concentrate to dryness. The crude product was diluted with 95% ethanol (30 mL) and filtered as a white solid to obtain Intermediate 1.

[0056] Intermediate 1 (10 mmol) and DIEA (20 mmol) were added to a solution of dichlorometha...

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Abstract

The invention relates to preparation and application of a dual-targeting ERK1 and ERK5 inhibitor, and belongs to the technical field of antitumor pharmacy. The technical problem to be solved by the invention is to provide a compound used as a double-targeting ERK1 and ERK5 inhibitor. The compound comprises a compound as shown in the specification or a pharmaceutically acceptable salt thereof. Thecompound or the pharmaceutically acceptable salt thereof can be used as an inhibitor of ERK1 and ERK5, has antitumor activity, and can effectively inhibit the growth of tumor cells. The compound is preferably an anti-tumor compound, and the characteristic of the corresponding tumor type is high expression of ERK1 and / or ERK5.

Description

technical field [0001] The invention relates to the preparation and application of a dual-target ERK1 and ERK5 inhibitor, belonging to the technical field of antitumor pharmacy. Background technique [0002] Tumor is one of the main chronic diseases that affect health, seriously affects the healthy life of human beings, and brings a heavy burden to society and families. Surgical resection combined with radiotherapy and chemotherapy will bring great harm to the patient's body and mind. Targeted therapy is a new type of treatment method, which has the advantages of clear targets, few side effects, and can directly act on diseased tissues. It has become the first choice for tumor treatment. important research direction. At present, the most important problem facing tumor targeted therapy is the lack of alternative drug targets and the lack of research on corresponding targeted small molecules. Therefore, discovering new therapeutic targets and designing targeted drugs are impo...

Claims

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Application Information

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IPC IPC(8): C07D495/04A61P35/00A61K31/4365A61K31/506A61K31/444
CPCC07D495/04A61P35/00
Inventor 欧阳亮王贯赵玉倩
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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