野艾蒿内酯I衍生物及其药物组合物和其制备方法与应用

By modifying the structure of Artemisia lactone I to synthesize a new derivative, the problem of the lack of effective liver cancer drugs in the existing technology is solved, and a new compound with stronger inhibitory activity and better safety is provided, which is suitable for industrial production.

CN118184675BActive Publication Date: 2026-07-17KUNMING INST OF BOTANY CHINESE ACAD OF SCI

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
KUNMING INST OF BOTANY CHINESE ACAD OF SCI
Filing Date
2024-03-15
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

There is a lack of effective artemisia lactone I derivatives and their drug compositions for the treatment of liver cancer in the current technology, and existing drugs have problems such as obvious toxic side effects and high price.

Method used

A series of new derivatives 1-33 were synthesized by structural modification of Artemisia lactone I and prepared into pharmaceutical compositions. Using palladium acetate, iodobenzene, sodium hypochlorite, and 4-methylbenzaldehyde oxime as catalysts and reactants, coupling, cycloaddition, esterification, and Diels-Alder reactions were carried out to prepare compounds with anti-hepatocellular carcinoma activity.

Benefits of technology

This study provides novel compounds with stronger inhibitory activity and better safety. Some derivatives have shown stronger inhibitory effects on liver cancer cells than existing drugs. Furthermore, the synthetic routes are short and the yields are high, making them suitable for industrial production.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明提供结构式(I)所示33个野艾蒿内酯I衍生物1‑33及其药物组合物和其制备方法与应用,属于药物技术领域。本发明的野艾蒿内酯I衍生物1‑33对人肝癌细胞株(HepG2,Huh7,SK‑Hep‑1)具有明显的抑制活性,能够与可药用载体组成药物组合物,能够用于制备抗肝癌药物。
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