Synthesis and biological evaluation of boronated nucleosides for boron neutron capture therapy (BNCT) of cancer

Authors
Tjarks, W Wang, J Chandra, S Ji, W Zhuo, J Lunato, AJ Boyer, C Li, Q Usova, EV Eriksson, S Morrison, GH Cosquer, GY
Citation
W. Tjarks et al., Synthesis and biological evaluation of boronated nucleosides for boron neutron capture therapy (BNCT) of cancer, NUCLEOS NUC, 20(4-7), 2001, pp. 695-698
Citations number
8
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
ISSN journal
15257770 → ACNP
Volume
20
Issue
4-7
Year of publication
2001
Pages
695 - 698
Database
ISI
SICI code
1525-7770(2001)20:4-7<695:SABEOB>2.0.ZU;2-H
Abstract
Several N-3 substituted carboranyl Thd analogs were synthesized. These agen ts as well as some non-boronated nucleosides were evaluated in, phosphoryl transfer assays with recombinant human TK1 and TK2. For some carboranyl thy midine analogs, TK1 phosphorylation rates approached 38% that of thymidine. Their in vitro cytotoxicty appeared to correlate with the TK1 levels in th e tested cells. In some cases increased uptake in tumor cell nuclei compare d with the surrounding cytoplasm was detected in vitro.