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

Autor:	Tjarks W; Ohio State University, College of Pharmacy, 500 W. 12th Ave, Columbus, Ohio 43210, USA. tjarks.l@osu.edu, Wang J, Chandra S, Ji W, Zhuo J, Lunato AJ, Boyer C, Li Q, Usova EV, Eriksson S, Morrison GH, Cosquer GY
Jazyk:	angličtina
Zdroj:	Nucleosides, nucleotides & nucleic acids [Nucleosides Nucleotides Nucleic Acids] 2001 Apr-Jul; Vol. 20 (4-7), pp. 695-8.
DOI:	10.1081/NCN-100002353
Abstrakt:	Several N-3 substituted carboranyl Thd analogs were synthesized. These agents as well as some non-boronated nucleosides were evaluated in phosphoryl transfer assays with recombinant human TK1 and TK2. For some carboranyl thymidine analogs, TK1 phosphorylation rates approached 38% that of thymidine. Their in vitro cytotoxicty appeared to correlate with the TK1 levels in the tested cells. In some cases increased uptake in tumor cell nuclei compared with the surrounding cytoplasm was detected in vitro.
Databáze:	MEDLINE
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