Anomeric sugar boronic acid analogues as potential agents for boron neutron capture therapy

Abstract

After the development of accelerators as neutron source, the access to new suitable agents for boron neutron capture therapy (BNCT) became a major need. Among many others, sugar boronic acids have recently attracted attention as boron carriers. Herein we report the synthesis and preliminary biological studies of two new sugar analogues containing a boronic acid at the anomeric position. The analogues were obtained by hydroboration of proper open-chain terminal alkenes that, after quenching with water, spontaneously afforded cyclic boronic acids with hemiacetal-like structures.

Keywords

• antitumor agents
• boron neutron capture therapy
• boronic acid
• hydroboration
• sugar analogue