A new inhibitor of pyrimidine phosphorylases

Authors
Dmitrieva, NA Molchan, OK Komissarov, AA Sokolov, VB Aksinenko, AY Pushin, AN Chekhlov, AN Debabov, VG
Citation
Na. Dmitrieva et al., A new inhibitor of pyrimidine phosphorylases, BIOORG KHIM, 24(12), 1998, pp. 920-925
Citations number
37
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANICHESKAYA KHIMIYA
ISSN journal
01323423 → ACNP
Volume
24
Issue
12
Year of publication
1998
Pages
920 - 925
Database
ISI
SICI code
0132-3423(199812)24:12<920:ANIOPP>2.0.ZU;2-5
Abstract
5,5-Bis(hydroxymethyl)-2-oxo-[1-(2-trifluoromethyl)-3,3,3-trifluoropropiona mido)-1-trifluoromethyl-2,2,2-trifluoroethyl-1,3,2-dioxaphosphan (CA-423) i s an in vitro inhibitor of the Escherichia coli uridine and thymidine phosp horylases. Unlike widely studied nucleoside analogues, this compound binds to the enzymes irreversibly. Its LD50 in mice was 40 mg/kg. Due to the invo lvement of pyrimidine phosphorylases in carcinogenesis and the relatively l ow toxicity of CA-423, it Is promising for anticancer therapy.