Aryl ketone derivative and furazan spliced conjugate as well as preparation method and application thereof

By designing conjugates that are spliced with aryl ketone derivatives and furazole, the shortcomings of existing anti-tumor drugs in inhibiting P-gp overexpression resistant tumor cells were solved, high selective inhibition and good water solubility were achieved, and new anti-tumor drug development ideas were provided.

CN120329263APending Publication Date: 2025-07-18FUDAN UNIVERSITY
0 Cites 0 Cited by

Patent Information

Application Number
CN202510487000.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-04-18
Publication Date
2025-07-18

AI Technical Summary

Technical Problem

Existing anti-tumor drugs are difficult to effectively inhibit multidrug-resistant tumor cells caused by P-gp overexpression, and traditional drugs are poor in water solubility, making it difficult to function in the body.

Method used

A conjugate of aryl ketone derivatives and furazole was designed and synthesized, and MDR tumor cells with P-gp overexpression were selectively inhibited through the nitric oxide donor mechanism, and synthesized using specific catalysts and reaction steps, improving the water solubility and anti-tumor activity of the compound.

Benefits of technology

High selective inhibition of drug-resistant tumor cells overexpressed by P-gp was achieved, the water solubility of the compound was increased by 24-775 times, and it showed significant antiproliferative activity against multidrug-resistant tumor cells, and was low in normal cytotoxicity.

✦ Generated by Eureka AI based on patent content.
Patent Text Reader

Abstract

The invention relates to the field of chemical pharmacy, in particular to an aryl ketone derivative and furazan spliced conjugate as well as a preparation method and application thereof. The structural formula of the conjugate spliced by the aryl ketone derivative and the furazan is as shown in any one of formulas I-V: # imgabs0 # imgabs1 #. A coumarin skeleton is opened, and the conjugate spliced by the aryl ketone derivative and the furazan is designed and synthesized. The aryl ketone derivative and furazan combined conjugate disclosed by the invention is novel in structure, has the effect of highly selectively inhibiting the proliferation activity of P-gp overexpression drug-resistant tumor cells, and provides a new thought and direction for overcoming the multidrug resistance of the tumor cells caused by P-gp overexpression.
Need to check novelty before this filing date? Find Prior Art