Boron
neutron capture therapy (BNCT) is a binary therapeutic approach.
Nonradioactive boron-10 atoms accumulated in tumor cells combining
with the neutron beams produce two highly energetic particles that
could eradicate the cell that takes it and the neighboring cells.
Small molecules that carry boron atom, e.g. 5- and 6-boronated and
2,7-diboronated tryptophans, were assessed for their boron accumulation
in U87-MG, LN229, and 3T3 for BNCT. TriBoc tryptophan, TB-6-BT, shows
boron-10 at 300 ppm in both types of tumor cells with a tumor to normal
ratio (T/N) of 5.19–5.25 (4 h). TB-5-BT and DBA-5-BT show boron-10
at 300 ppm (2 h) in U87-MG cells. TB-5-BT exerts a T/N of >9.66
(1
h) in LN229 compared with the current clinical boronophenyl alanine
with a highest T/N of 2.3 (1 h) and accumulation concentration of
<50 ppm. TB-5-BT and TB-6-BT warrant further animal study.
The data presented in this article are related to the research article entitled “Synthesis and Characterization of Boron Fenbufen and its F-18 Labeled Homolog for Boron Neutron Capture Therapy of COX-2 Overexpressed Cholangiocarcinoma”. The contents of the data article include 1) the set up for performing in vitro binding assay, 2) 1H-, 13C- and 19F-NMR of compounds described in main text, 3) HPLC chromatogram of the fluorination mixtures, 4) data of in vitro stability test, cell survival assay, western blot and PCR analysis, 5) the modules for fixing the two CCA rats for BNCT, and 6) bar diagram for tumor reduction using [18F]FDG-PET 24 h post treatment with BNCT.
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