Dihydroartemisinin-amine derivative, and preparation method and application thereof

By modifying the structure of the alkylation moiety of nitrogen mustard and linking it with DHA, dihydroartemisinin-amine derivatives were synthesized, solving the problems of drug resistance and toxic side effects of existing antitumor drugs, and achieving highly efficient inhibition of human lung cancer cells and low toxicity to normal cells.

CN117756817BActive Publication Date: 2026-06-12NINGXIA UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2023-12-18
Publication Date
2026-06-12

AI Technical Summary

Technical Problem

Existing anti-tumor drugs have drug resistance and toxic side effects, affecting immunity and causing damage to the defense system, especially when treated with high doses of anticancer drugs.

Method used

By structurally modifying the alkylation portion of nitrogen mustard, a series of dihydroartemisinin-amine derivatives were synthesized. Utilizing molecular hybridization theory and the principle of synergistic activity, the toxic side effects of nitrogen mustard were reduced and its anticancer activity was enhanced. Compounds with potential anticancer activity were prepared by one-pot reaction and fluorination of DHA with secondary amine compounds in a specific solvent.

Benefits of technology

It significantly improved the inhibitory activity against human lung cancer cells and reduced the toxicity to normal cells. The selectivity coefficient of compound 3d was much higher than that of the existing positive control, which has important application value for anti-lung cancer drugs.

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Abstract

The embodiment of the application discloses a dihydroartemisinin-amine derivative and a preparation method and application thereof.The structure of the dihydroartemisinin-amine derivative is shown as formula (I), wherein R 3 is selected from a hydrocarbon group or a substituted hydrocarbon group.A series of secondary amine compounds with nitrogen mustard as a template are synthesized, and are further connected with dihydroartemisinin (DHA) to obtain a series of dihydroartemisinin-amine derivatives with good activity and low toxic side effects, and the dihydroartemisinin-amine derivatives have good application prospects in anticancer.
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Citation Information

Patent Citations

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