Dm. Adams et al., Comparative in vitro evaluation of dequalinium B, a new boron carrier for neutron capture therapy (NCT), ANTICANC R, 20(5B), 2000, pp. 3395-3402
A boronated derivative of dequalinium, a delocalized lipophilic cation (DLC
), was synthesized as a potential boron carrier for the selective targeting
of mitochondria in malignant versus benign cells for boron neutron capture
therapy (BNCT), a binary modality for the treatment of cancer. This agent,
designated DEQ-B, was taken lip and retained in vitro in the KB, F98, and
C6 tumor cell lines but not in the normal epithelial cell line CVI. DEQ-B w
as also less toxic in the latter cell fine at lower exposure concentrations
The uptake, retention, and toxicity profiles of DEQ-B ate comparable to th
ose of the non-boronated DLCs, dequalinium, MKT 077, RH 123, and tetrapheny
lphosphonium chloride. Our results suggest that the synthesis and further e
valuation of boronated DLCs as potential delivery agents for BNCT is warran
ted.