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

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2021 Jun 2

PMID 34077212

Citations 2

Authors

Hiroki Ueda

Minoru Suzuki

Reiko Kuroda

Tomohiro Tanaka

Shin Aoki

Affiliations

Soon will be listed here.

Abstract

Boron neutron capture therapy (BNCT) is a binary therapeutic method for cancer treatment based on the use of a combination of a cancer-specific drug containing boron-10 (B) and thermal neutron irradiation. For successful BNCT, B-containing molecules need to accumulate specifically in cancer cells, because destructive effect of the generated heavy particles is limited basically to boron-containing cells. Herein, we report on the design and synthesis of boron compounds that are functionalized with 9-, 12-, and 15-membered macrocyclic polyamines and their Zn complexes. Their cytotoxicity, intracellular uptake activity into cancer cells and normal cells, and BNCT effect are also reported. The experimental data suggest that mono- and/or diprotonated forms of metal-free [12]aneN- and [15]aneN-type ligands are uptaken into cancer cells, and their complexes with intracellular metals such as Zn would induce cell death upon thermal neutron irradiation, possibly via interactions with DNA.

Citing Articles

Novel Drug Delivery Particles Can Provide Dual Effects on Cancer "Theranostics" in Boron Neutron Capture Therapy.

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Advances in the synthesis and applications of macrocyclic polyamines.

Gao Y, Guo L, Liu X, Chen N, Yang X, Zhang Q R Soc Open Sci. 2024; 11(6):231979.

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