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

Bai Chuan Pan, Zhi Hao Chen, Edward Chu, Ming Yu WangChu, Shih Hsi Chu

Research output: Contribution to journalArticlepeer-review

10 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)2367-2382
Number of pages16
JournalNucleosides and Nucleotides
Volume17
Issue number12
DOIs
StatePublished - 1998
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Genetics

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