Preparation of 10B-enriched nitroimidazole derivative by click reaction as a functional drug for hypoxia-targeting boron-neutron capture therapy
We report a novel drug that can be used for the treatment of tumor hypoxic cells by boron neutron capture therapy. We attempted to modify p‑boronophenylalanine, a agent for this therapy in practical use, with a hypoxia-accumulating functional group, 2-nitroimidazole derivative to form p‑boronophenyl...
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| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Elsevier
2025-05-01
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| Series: | Results in Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S2211715625002280 |
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| Summary: | We report a novel drug that can be used for the treatment of tumor hypoxic cells by boron neutron capture therapy. We attempted to modify p‑boronophenylalanine, a agent for this therapy in practical use, with a hypoxia-accumulating functional group, 2-nitroimidazole derivative to form p‑boronophenylalanine with nitroimidazole group (BPA-NI). We successfully prepared 10B-enriched BPA-NI by using click chemistry between azide-modified p‑boronophenylalanine and alkyne-modified nitroimidazole in the presence of copper catalysis. This functional molecule showed selective accumulation in hypoxic cells, and therefore showed robust cytotoxic effects toward hypoxic cells upon thermal neutron irradiation. |
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| ISSN: | 2211-7156 |