A kind of tetrapeptide propylene oxide derivative and its preparation method and use

A technology of peptide propylene oxide and propylene oxide, which is applied to novel tetrapeptide propylene oxide derivatives and their application fields in pharmacodynamics, and can solve problems such as toxic and side effects

Active Publication Date: 2020-08-21
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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  • A kind of tetrapeptide propylene oxide derivative and its preparation method and use
  • A kind of tetrapeptide propylene oxide derivative and its preparation method and use
  • A kind of tetrapeptide propylene oxide derivative and its preparation method and use

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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

Disclosed in the present invention are a tetrapeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, as well as a preparation method therefor, and the use thereof. The structure of the tetrapeptide propylene oxide derivative or the pharmaceutically acceptable salt thereof is shown in formula I. The compound of the present invention can selectively inhibit the chymotrypsin-like activity of 20S proteasome, and is also expected to display anti-inflammatory properties and inhibition of cell proliferation.

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 Patents(China)
IPC IPC(8): C07K7/06C07K5/107C07K5/103C07K5/117C07K1/06A61K38/08A61K38/07A61P29/00A61P35/00A61P37/02
CPCA61K38/00C07K5/1008C07K5/101C07K5/1013C07K5/1016C07K5/1024C07K7/06
Inventor 朱永强雷萌张浩洋杜晓
Owner NANJING LINGRUI PHARM TECH CO LTD
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