Issue 79, 2021

Carboxyboranylamino ethanol: unprecedented discovery of boron agents for neutron capture therapy in cancer treatment

Abstract

Carboxyboranylamino ethanol (Me2N(BH2CO2H)CH2CH2OH, 1) was prepared in 75.0% yield by an amine-exchange reaction. Compound 1 shows lower cytotoxicity and higher anti-tumor efficacy in vitro towards the SCCVII cell line in comparison with 4-borono-L-phenylalanine (BPA) and methyl 2-hydroxyl-5-(1′-ortho-carbonylmethyl-1′,2′,3′-triazol-4′-yl)-benzonate (2). The bio-enhancement is interpreted using molecular docking calculations.

Graphical abstract: Carboxyboranylamino ethanol: unprecedented discovery of boron agents for neutron capture therapy in cancer treatment

Supplementary files

Article information

Article type
Communication
Submitted
17 juin 2021
Accepted
08 sept. 2021
First published
10 sept. 2021

Chem. Commun., 2021,57, 10174-10177

Carboxyboranylamino ethanol: unprecedented discovery of boron agents for neutron capture therapy in cancer treatment

Y. Zhu, J. Cai, N. S. Hosmane, M. Suzuki, K. Uno, Y. Zhang and M. Takagaki, Chem. Commun., 2021, 57, 10174 DOI: 10.1039/D1CC03034E

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