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Tripeptide propylene oxide derivative and preparation method and application thereof

A technology of peptide propylene oxide and propylene oxide, applied in the field of novel tripeptide propylene oxide derivatives and their preparation, can solve problems such as toxic and side effects

Active Publication Date: 2019-08-06
SHENZHEN JIKANG 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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  • Tripeptide propylene oxide derivative and preparation method and application thereof
  • Tripeptide propylene oxide derivative and preparation method and application thereof
  • Tripeptide propylene oxide derivative and preparation method and application thereof

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Experimental program
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Embodiment Construction

[0118] The technical solutions of the present invention will be further described below through specific embodiments.

[0119] Synthesis of the first part of the compound

[0120] The preparation of the compound of the present invention can be carried out according to the following process:

[0121] One, the preparation of compound (II)

[0122]

[0123] 1. Preparation of compound (II-3):

[0124] Dissolve compound (II-1), HOBt in anhydrous DCM and stir at -5°C for 10 min, then add EDI·HCl at this temperature, stir for 15-20 min, then add compound (II-2) and stir for 15-20 min, Then DIPEA was added and stirred for 20 minutes, then moved to room temperature for reaction. After the reaction is complete, pour into water, extract with DCM, combine the organic phases with dilute HCl, NaHCO 3 The solution was washed with saturated brine, dried over anhydrous sodium sulfate, and evaporated to dryness to obtain compound (II-3).

[0125] 2. Preparation of compound (II-4):

[0...

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PUM

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Abstract

The invention discloses a tripeptide propylene oxide derivative and a preparation method and application thereof. The structure of the tripeptide ethylene oxide derivative is shown as the formula I. Compared with the prior art, the invention provides a tripeptide epoxy ketone compound being novel in structure and having function of restraining proteasome, which are used as a 20S proteasome inhibitor to block tumor cell proliferation and induce tumor apoptosis so as to be used for treating and preventing people and animals from suffering from multiple diseases such as malignant tumors. The effect is notably better.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a novel tripeptide propylene oxide derivative, a preparation method thereof and an application in pharmacy. 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 degen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/087C07K5/097C07K5/117C07K1/06A61K38/06A61K38/07A61P35/00
CPCC07K5/0812C07K5/0821C07K5/1024A61P35/00A61K38/00A61K38/06C07K5/0606C07K5/081C07K5/08
Inventor 朱永强雷萌张浩洋
Owner SHENZHEN JIKANG PHARM TECH CO LTD
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