Synthesis of 5-Halogeno-6-amino-2′-deoxyurldines and their Analogs as Potential Inhibitors of Thymidine Phosphorylase

Autor: Ming Yu WangChu, Bai Chuan Pan, Shih Hsi Chu, Zhi Hao Chen, Edward Chu
Rok vydání: 1998
Předmět:
Zdroj: Nucleosides and Nucleotides. 17:2367-2382
ISSN: 0732-8311
DOI: 10.1080/07328319808004324
Popis: 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.
Databáze: OpenAIRE