Flavonoid derivatives and their preparation method and application

By preparing flavonoid derivatives to form salts with specific acids, the problem of flavonoid compounds being poorly soluble in water is solved, and targeted treatment of tumors and autoimmune diseases with abnormal STAT3 is achieved, with significant anti-cancer and immunomodulatory effects.

CN119219591BActive Publication Date: 2025-09-16HENAN RADIOMEDICAL SCI & TECH CO LTD +1
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Patent Information

Application Number
CN202411232310.6
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2024-09-04
Publication Date
2025-09-16
Estimated Expiration
2044-09-04

AI Technical Summary

Technical Problem

Existing flavonoids are poorly soluble in water, which limits their pharmacological activity and makes it difficult to effectively target and treat tumors associated with STAT3 overexpression and abnormal activation.

Method used

A class of flavonoid derivatives are synthesized and formed into biologically acceptable salts with acetic acid, dihydrofolic acid, benzoic acid, etc., and small molecule compounds with targeted anti-tumor activity are prepared through a specific chemical reaction route.

Benefits of technology

It effectively inhibits diseases related to abnormal STAT3 signaling, including various tumors and autoimmune diseases, significantly inhibits the proliferation of related cells, and downregulates STAT3 activation and downstream target protein expression, with good anti-cancer effects.

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Abstract

The present invention discloses a class of flavonoid derivatives, their preparation methods, and applications. The structural formula is shown in Formula I: wherein X is selected from CH and N, and R1 is selected from H. These compounds can significantly inhibit the activation of STAT3, a cell signaling pathway, at low doses. Experimental results show that these compounds can significantly inhibit the proliferation of various tumor cell lines, including lymphoma, multiple myeloma, cervical cancer, breast cancer, gastric cancer, lung cancer, and pancreatic cancer. They can specifically inhibit STAT3 signaling activation and the expression of the downstream target gene cyclinD1, indicating that these compounds have the potential to be developed as targeted anti-tumor drugs related to the STAT3 signaling pathway.
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