1,5-diaryl-1,2,4-triazole derivatives targeting myoferlin and synthesis and use thereof

By designing 1,5-diaryl-1,2,4-triazole compounds with nitrogen-containing five-membered heterocyclic structures, the problem of insufficient water solubility of Myoferlin targeted drugs was solved, and efficient inhibition of tumor cell proliferation and migration was achieved under various pH conditions, showing broad potential for anti-tumor applications.

CN119528884BActive Publication Date: 2025-12-05EAST CHINA NORMAL UNIV
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Patent Information

Application Number
CN202311104918.6
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-08-30
Publication Date
2025-12-05
Estimated Expiration
2043-08-30

AI Technical Summary

Technical Problem

Existing targeted drugs have insufficient water solubility for Myoferlin, which affects its drug-like properties under various pH conditions and makes it difficult to effectively inhibit the proliferation and migration of tumor cells.

Method used

A novel class of 1,5-diaryl-1,2,4-triazole compounds was designed and synthesized. By introducing a nitrogen-containing five-membered heterocyclic structure, the water solubility of the compounds under different pH conditions was significantly improved, and their binding ability to Myoferlin protein was enhanced.

Benefits of technology

It significantly improved the water solubility of the compound under pH conditions of 2.0, 7.4 and 9.0, enhanced the drug-likeness of the drug, and effectively inhibited the proliferation and migration of various cancer cells, showing broad prospects for anti-tumor applications.

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Abstract

The application discloses a kind of 1,5-diaryl-1,2,4-triazole compounds or pharmaceutically acceptable salt represented by structural formula I, II or pharmaceutical composition containing such compounds.The application also discloses the application of the compound or pharmaceutically acceptable salt in the preparation of drugs for treating various malignant tumors and related diseases of tumor metastasis.The compound represented by formula I, II of the application can inhibit the proliferation, invasion and infiltration of tumor cells such as gastric cancer cells, breast cancer cells, prostate cancer cells, colon cancer cells, liver cancer cells, non-small cell lung cancer cells and bladder cancer cells in a concentration gradient-dependent manner, has the characteristics of high efficiency and low toxicity, and has a wide application prospect in the biological medicine industry.
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