A class of piperazineamide derivatives and their preparation method and application

By synthesizing piperazineamide derivatives with a completely new structure, the problem of existing STAT3 inhibitors not being available on the market was solved, and the proliferation inhibition of various tumor cells and STAT3 signal inhibition were achieved, with significant anti-cancer effects.

CN118702675BActive Publication Date: 2025-09-05HENAN RADIOMEDICAL SCI & TECH CO LTD
2 Cites 0 Cited by

Patent Information

Application Number
CN202410707213.1
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-06-03
Publication Date
2025-09-05
Estimated Expiration
2044-06-03

AI Technical Summary

Technical Problem

Existing STAT3 inhibitors have not yet been successfully marketed, and there is an urgent need to develop anti-tumor drugs that directly target STAT3 to inhibit the growth and metastasis of various tumor cells.

Method used

A new class of piperazine amide derivatives with a novel structure has been synthesized. By forming biologically acceptable salts with a variety of acids, they significantly inhibit the activation of STAT3 signals. The preparation method includes a multi-step chemical synthesis route and has been applied to inhibit the proliferation of various tumor cells.

Benefits of technology

Piperazineamide derivatives effectively inhibit the proliferation of lymphoma, multiple myeloma, leukemia, breast cancer, gastric cancer, lung cancer and pancreatic cancer cells, and significantly inhibit STAT3 signal transduction, showing good anti-cancer effects.

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

Abstract

The present invention discloses a class of piperazinamide derivatives, their preparation methods, and applications, belonging to the field of targeted tumor therapeutics. The structural formula is shown in General Formula I: #imgabs0#, wherein n=1, 2, 3, 4, 5, ..., 10, and R1 is selected from #imgabs1##imgabs2#. These compounds can significantly inhibit the activation of the STAT3 signaling pathway in cell signaling at low doses. Experimental results show that these compounds can significantly inhibit the proliferation of various tumor cell lines, including lymphoma, multiple myeloma, leukemia, breast cancer, gastric cancer, lung cancer, and pancreatic cancer. They can specifically inhibit STAT3 signaling activation and the expression of the downstream target gene C-myc, indicating that these compounds have the potential to be developed as targeted anti-tumor drugs related to the STAT3 signaling pathway.
Need to check novelty before this filing date? Find Prior Art