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

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
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
ISSN journal
1525-7770 → 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.