A new class of drugs for BNCT? Borylated derivatives of ferrocenium compounds in animal experiments.

Abstract

A new class of drugs, borylated derivatives of ferrocenium compounds, which show a comparatively facile synthesis is investigated on their boron neutron capture accumulation. Investigations focused on the fast and effective testing of 12 ferrocene derivatives with tetracoordinated boron atoms, which should accumulate in rodent tumors. The macroscopic studies on time-dependent boron distributions and boron concentrations in mice were carried out by inductively coupled plasma-atomic emission spectrometry, inductively coupled plasma-mass spectrometry, and quantitative neutron capture radiography. The determination of boron concentrations after injection of 2b showed high boron contents in spleen, liver, kidneys, less in lung and muscle, and poor in integral blood, blood plasma, tumor, and brain. It is interesting to note that 2b penetrates the blood-brain barrier which may be advantageous in the treatment of astrocytomas and glioblastomas.