Fluorodeoxyuridine monophosphate prodrug and application thereof in preparation of medicine for treating liver cancer

By combining a novel fluorodeoxyuridine monophosphate prodrug with taraxasterol, the problems of low bioavailability and high toxicity of 5-FU in the treatment of liver cancer were solved, achieving a highly efficient and selective therapeutic effect for liver cancer.

CN121673349APending Publication Date: 2026-03-17BEIJING SHENLANTAI PHARM TECH CO LTD
1 Cites 0 Cited by

Patent Information

Application Number
CN202511907014.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-12-17
Publication Date
2026-03-17

AI Technical Summary

Technical Problem

Existing methods for treating liver cancer with 5-FU suffer from low bioavailability, high toxicity, poor tumor targeting, and drug resistance. Furthermore, the activity and selectivity of existing fluorodeoxyuridine monophosphate prodrugs need to be optimized.

Method used

A series of novel fluorodeoxyuridine monophosphate prodrugs were designed and synthesized, and used in combination with taraxasterol. By regulating the expression of HINT1 protein in tumor cells, the prodrugs were "activated in situ" in hepatocytes and achieved a synergistic anti-tumor effect.

Benefits of technology

It significantly improved the in vitro anti-hepatocellular carcinoma activity of fluorodeoxyuridine monophosphate prodrug, reduced its toxicity to normal hepatocytes, enhanced the therapeutic effect of hepatocellular carcinoma, and showed a synergistic anti-tumor effect when used in combination with taraxasterol.

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

Abstract

The invention discloses a fluorodeoxyuridine monophosphate prodrug as shown in a formula I, application of the prodrug in preparation of a medicine for treating liver cancer, a pharmaceutical composition containing the prodrug and pharmaceutically acceptable auxiliary materials or taraxasterol and application of the prodrug in preparation of the medicine for treating liver cancer, and belongs to the field of pharmacy. The compound is modified by specific natural amino acid residues and can be used for preparing medicines for treating liver cancer. The in-vitro and in-vivo anti-tumor activity of the compound is remarkably superior to that of the prior art, the compound has a synergistic effect when being combined with taraxasterol, the highest tumor inhibition rate reaches 91.72%, the compound is high in selectivity, good in safety and high in liver targeting performance, and a more effective new scheme is provided for liver cancer treatment.
Need to check novelty before this filing date? Find Prior Art