Synthesis of 5-halogeno-6-amino-2'-deoxyuridines and their analogs as potential inhibitors of thymidine phosphorylase

Article abstract of DOI:10.1080/07328319808004324

5-Halogeno-6-amino-2'-deoxyuridines were synthesized from 2'- deoxyuridine as potential thymidine phosphorylase (ThdPase) inhibitors. Among the compounds synthesized, 5-bromo-6-amino-2'-deoxyuridine (6) and 5-iodo-6- amino-2'-deoxyuridine (9) were found to inhibit ThdPase activity with IC50 values of 1.3 μM and 6.5 μM, respectively. In vitro cell culture studies showed that compound (6) can significantly enhance the cytotoxic effects of 5-fluoro-2'-deoxyuridine against a human colon cancer HCT-8 cell line.

Full text of DOI:10.1080/07328319808004324

Nucleosides and Nucleotides
ISSN: 0732-8311 (Print) (Online) Journal homepage: http://www.tandfonline.com/loi/lncn19
Synthesis of 5-Halogeno-6-amino-2′-deoxyurldines
and their Analogs as Potential Inhibitors of
Thymidine Phosphorylase
Bai-Chuan Pan , Zhi-Hao Chen , Edward Chu , Ming-Yu WangChu & Shih-Hsi
Chu
To cite this article: Bai-Chuan Pan , Zhi-Hao Chen , Edward Chu , Ming-Yu WangChu & Shih-Hsi
Chu (1998) Synthesis of 5-Halogeno-6-amino-2′-deoxyurldines and their Analogs as Potential
Inhibitors of Thymidine Phosphorylase, Nucleosides and Nucleotides, 17:12, 2367-2382, DOI:
10.1080/07328319808004324
To link to this article: http://dx.doi.org/10.1080/07328319808004324
Published online: 16 Aug 2006.
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Date: 29 January 2016, At: 02:03