Trifluoromethylated temozolomide and derivatives thereof and methods of preparation and use

By developing trifluoromethylated temozolomide and its derivatives and combining them with ultrasound therapy, the drug resistance problem of glioma and melanoma has been solved, achieving highly efficient killing of tumor cells and low toxicity to normal cells, which has significant clinical application value.

CN120718024BActive Publication Date: 2025-11-25TIANJIN MEDICAL UNIV +2
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Patent Information

Application Number
CN202511186979.0
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-08-25
Publication Date
2025-11-25
Estimated Expiration
2045-08-25

AI Technical Summary

Technical Problem

In the current technology, gliomas and melanomas have high resistance to temozolomide treatment, there is a lack of effective second-line treatment drugs, and traditional temozolomide has high toxicity to normal neurons during treatment.

Method used

Develop trifluoromethylated temozolomide and its derivatives, and combine them with ultrasound for sonodynamic therapy. By adjusting the drug structure and treatment method, the aim is to enhance the killing effect on tumor cells and reduce the toxicity to normal cells.

Benefits of technology

Trifluoromethyltemozolomide exhibits better killing effect on tumor cells at low concentrations, can cross the blood-brain barrier, and significantly enhances efficacy when combined with ultrasound therapy, while reducing toxicity to normal neurons.

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Abstract

The application belongs to the field of antitumor drugs, and particularly relates to trifluoromethylated temozolomide and derivatives thereof, a preparation method and application. The trifluoromethylated temozolomide has a better killing effect on tumor cells relative to traditional temozolomide, has a lower toxic effect on normal neuron cells at a low concentration relative to temozolomide, and can penetrate the blood-brain barrier through animal experiments.
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