Piperlongumine derivative as well as preparation method and application thereof

Abstract

The invention discloses a piperlongumine derivative as well as a preparation method and application thereof, and belongs to the technical field of medical chemistry. The piperlongumine derivative isshown as a formula (I): the piperlongumine derivative, as well as any mixture of these forms or a pharmaceutically acceptable salt thereof, can be used as the target Keap1 molecular probe, can position and bind the Keap1 protein in a lysis solution, and can be detected in the Western-Blot at the later stage so as to provide the new means for the research of the anti-tumor effect mechanism of the piperlongumine. According to the method, 3-hydroxy-4-nitrobenzaldehyde is used as a raw material, the synthesis process is simple, efficient and rapid, and the prepared piperlongumine derivative has relatively high yield.

Description

technical field

[0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a perylene amide derivative and a preparation method and application thereof. Background technique

[0002] Piperlongumine (Piperlongumine, PL) is an active natural product isolated and extracted from the Piper genus plant, and it has been found to have a variety of biological activities, such as anti-inflammatory, anti-fungal, treatment of anxiety and depression, anti-platelet aggregation and anti-tumor effects Wait. Studies have found that Piperamide selectively kills tumor cells and has very little toxicity to normal cells. This unique selective effect has attracted the attention of drug researchers at home and abroad, and it is used as a lead compound to research and develop new anti-tumor drugs.

[0003] The anti-tumor mechanism of Piperamide is still unclear, and it is widely considered as a class of small molecules that act on multiple targets, suc...

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