SYNTHESIS OF 5-HALOGENO-6-AMINO-2'-DEOXYURIDINES AND THEIR ANALOGS ASPOTENTIAL INHIBITORS OF THYMIDINE PHOSPHORYLASE

Authors
PAN BC CHEN ZH CHU E CHU MYW CHU SH
Citation
Bc. Pan et al., SYNTHESIS OF 5-HALOGENO-6-AMINO-2'-DEOXYURIDINES AND THEIR ANALOGS ASPOTENTIAL INHIBITORS OF THYMIDINE PHOSPHORYLASE, Nucleosides & nucleotides, 17(12), 1998, pp. 2367-2382
Citations number
30
Categorie Soggetti
Biology
Journal title
Nucleosides & nucleotides → ACNP
ISSN journal
07328311
Volume
17
Issue
12
Year of publication
1998
Pages
2367 - 2382
Database
ISI
SICI code
0732-8311(1998)17:12<2367:SO5ATA>2.0.ZU;2-T
Abstract
5-Halogeno-6-amino-2'-deoxyuridines were synthesized from 2'-deoxyurid ine as potential thymidine phosphorylase (ThdPase) inhibitors. Among t he compounds synthesized, 5-bromo-6-amino-2'-deoxyuridine (6) and 5-io do-6-amino-2'-deoxyuridine (9) were found to inhibit ThdPase activity with IC50 values of 1.3 mu M and 6.5 mu M, respectively. In vitro cell culture studies showed that compound (6) can significantly enhance th e cytotoxic effects of 5-fluoro-2'-deoxyuridine against a human colon cancer HCT-8 cell line.