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Tetrapeptide epoxy propane derivative, preparation method and application thereof

A technology of peptide propylene oxide and propylene oxide, which is applied in the field of new tetrapeptide propylene oxide derivatives and its application in pharmacodynamics, and can solve problems such as toxic and side effects

Active Publication Date: 2017-07-14
NANJING LINGRUI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the anticancer drugs currently on the market have certain curative effects, most of them are cytotoxic drugs with serious toxic and side effects

Method used

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  • Tetrapeptide epoxy propane derivative, preparation method and application thereof
  • Tetrapeptide epoxy propane derivative, preparation method and application thereof
  • Tetrapeptide epoxy propane derivative, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0117] Synthesis of the first part of the compound

[0118] The preparation of the compound of the present invention can be carried out according to the following process:

[0119] One, the preparation of compound (I)

[0120]

[0121] 1. Preparation of compound (I-3):

[0122] Dissolve compound (I-1), HOBt in anhydrous DCM and stir at -5°C for 10 min, then add EDIHCl at this temperature, stir for 15-20 min, then add compound (I-2) and stir for 15-20 min, then add DIPEA was stirred for 20 minutes, then moved to room temperature for reaction. After the reaction was complete, it was poured into water, extracted with DCM, and the combined organic phases were washed with dilute HCl, sodium bicarbonate solution, and saturated brine, dried over anhydrous sodium sulfate, and evaporated to dryness to obtain compound (I-3).

[0123] 2. Preparation of compound (I-4):

[0124] Compound (I-3) was dissolved in anhydrous DCM, TFA was slowly added dropwise at -5°C, stirred for 0.5 hou...

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Abstract

The invention discloses a tetrapeptide epoxy propane derivative or a pharmaceutically acceptable salt thereof, and a preparation method and an application thereof, wherein the tetrapeptide epoxy propane derivative or the pharmaceutically acceptable salt thereof is represented as the formula (I). The compound can selectively inhibit chymotrypsin like activity of 20S proteasome, and also may have anti-inflammation feature and cell proliferation inhibition effect.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a novel tetrapeptide propylene oxide derivative and its application in pharmacodynamics. Background technique [0002] At present, malignant tumors are still one of the major diseases that threaten people's lives. Although the treatment of cancer has made great progress, it has not been able to treat cancer fundamentally. Although the currently marketed anticancer drugs have certain curative effects, most of them are cytotoxic drugs with serious toxic and side effects. Therefore, how to start from effective tumor targets to study targeted new anticancer drugs has become a top priority for medical workers. [0003] The Ubiquitin-Proteasome Pathway (UPP) can regulate the level of proteins involved in cell cycle control. This pathway has an important relationship with the pathogenesis of cancer, cardiovascular and cerebrovascular diseases and degenerative diseases of the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K5/107C07K5/103C07K5/117C07K1/06A61K38/08A61K38/07A61P29/00A61P35/00A61P37/02
CPCC07K5/1008C07K5/101C07K5/1013C07K5/1016C07K5/1024C07K7/06A61K38/00
Inventor 朱永强雷萌张浩洋杜晓
Owner NANJING LINGRUI PHARM TECH CO LTD
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