Design, Synthesis and Biological Evaluation of Boron-Containing Macrocyclic Polyamine Dimers and Their Zinc(II) Complexes for Boron Neutron Capture Therapy

Hiroki Ueda, Minoru Suzuki, Yoshinori Sakurai, Tomohiro Tanaka, Shin Aoki

研究成果: Article査読

抄録

Boron neutron capture therapy (BNCT) is considered to have potential for cancer therapy based on the nuclear reaction between boron (10B) atoms and thermal neutrons, yielding 4He2+ (α) and 7Li3+ ions. These heavy particles induce the destruction of biomolecules within short path length of 5–9 μm, resulting in a limited cytotoxic effect to 10B-containing cells. Herein, we report on the design and synthesis of DNA-targeting BNCT agents equipped with homo- and hetero-dimeric macrocyclic polyamine units and their Zn2+ complexes. It was hypothesized that the dizinc(II) complexes of these ligands would recognize two adjacent thymidines (thymidyl(3'–5')thymidine), resulting in an efficient contact with DNA and an efficient breakdown of DNA upon thermal neutron irradiation. To test this hypothesis, we performed a DNA interaction study and a biological evaluation such as cytotoxicity and intracellular uptake activity using cancer and normal cells. BNCT experiments utilizing the corresponding 10B-enriched compounds were also conducted.

本文言語English
論文番号e202100949
ジャーナルEuropean Journal of Inorganic Chemistry
2022
5
DOI
出版ステータスPublished - 16 2月 2022

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