A Hypoxia-Targeted Boron Neutron Capture Therapy Agent for the Treatment of Glioma.

ABSTRACT:

Purpose

Boron neutron capture therapy (BNCT) has the potential to become a viable cancer treatment modality, but its clinical translation has been limited by the poor tumor selectivity of agents. To address this unmet need, a boronated 2-nitroimidazole derivative (B-381) was synthesized and evaluated for its capability of targeting hypoxic glioma cells.

Methods

B-381 has been synthesized from a 1-step reaction. Using D54 and U87 glioma cell lines, the in vitro cytotoxicity and cellular accumulation of B-381 has been evaluated under normoxic and hypoxic conditions compared to L-boronophenylalanine (BPA). Furthermore, tumor retention of B-381 was evaluated in vivo.

Results

B-381 had low cytotoxicity in normal and cancer cells. Unlike BPA, B-381 illustrated preferential

SUBMITTER: Luderer MJ 

PROVIDER: S-EPMC5007153 | biostudies-literature | 2016 Oct

REPOSITORIES: biostudies-literature