Boron medicine with tumor targeted release capability for boron neutron capture therapy and preparation method thereof

The tumor-targeted boron drug synthesized through a new preparation method can activate and target release boron-10 drugs in tumor cells at high concentrations of NAD(P)H in tumor cells, solving multiple shortcomings of existing BNCT drugs in clinical applications and achieving efficient and safe treatment effects of boron neutron capture.

CN119751530APending Publication Date: 2025-04-04AFFILIATED HOSPITAL OF NANTONG UNIV +2
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Patent Information

Application Number
CN202411718164.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-11-28
Publication Date
2025-04-04

AI Technical Summary

Technical Problem

Existing boron neutron capture therapy (BNCT) drugs, such as boron phenylalanine (BPA) and thiodoborane dinanosaline (BSH), have problems in clinical applications with low water solubility, potential toxic side effects, inability to cross the blood-brain barrier, and low tumor uptake and retention capabilities.

Method used

A new preparation method is used to synthesize a boron drug with targeted release ability. It reacts with quinoline-3-methanol with halogenated reagents, and then reacts with triphosgene and boron-10 compounds to form a compound that can activate and target the release of boron-10 drugs in tumor cells at high concentrations of NAD(P)H.

Benefits of technology

This boron drug has the advantages of strong targeting, high biosafety, simple synthesis methods, mild conditions, high yield, stable chemical properties, good photostability and low toxicity. It can effectively improve the therapeutic effect of BNCT and reduce damage to normal cells.

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Abstract

The invention provides a boron drug with tumor targeted release capability for boron neutron capture therapy and a preparation method thereof, relates to the technical field of tumor therapy, and provides a boron drug which can be activated through high-concentration NAD (P) H at a tumor site and can release a B-10 drug in a targeted manner for boron neutron capture therapy. A boron-10-containing compound in the boron medicine is connected with 3-aldehyde quinoline salt through a self-elimination reactive group, the 3-aldehyde quinoline salt can be specifically reduced by NAD (P) H rich in tumor cells to trigger chain reaction, and the effective boron-10 compound is released for boron neutron capture therapy. The damage to normal cells in the BNCT process can be effectively reduced by a method for targeted aggregation of the boron drug in the tumor cells. The boron drug synthesis method is simple, mild in condition and high in yield, has the advantages of stable chemical property, good light stability, small toxicity and the like, and provides a good application prospect for the field of boron neutron capture therapy.
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