1. [A new inhibitor of pyrimidine phosphorylase].
- Author
-
Dmitrieva NA, Molchan OK, Komissarov AA, Sokolov VB, Aksinenko AIu, Pushin AN, Chekhlov AN, and Debabov VG
- Subjects
- Animals, Enzyme Inhibitors chemistry, Enzyme Inhibitors toxicity, Escherichia coli enzymology, Lethal Dose 50, Magnetic Resonance Spectroscopy, Mice, Organophosphorus Compounds chemistry, Organophosphorus Compounds toxicity, Propionates chemistry, Propionates toxicity, Enzyme Inhibitors pharmacology, Organophosphorus Compounds pharmacology, Propionates pharmacology, Thymidine Phosphorylase antagonists & inhibitors
- Abstract
5,5-Bis(hydroxymethyl)-2-oxo-[1-(2-trifluoromethyl)-3,3,3- trifluoropropionamido)-1-trifluoromethyl-2,2,2-trifluoroethyl- 1,3,2-dioxaphosphan (CA-423) is an in vitro inhibitor of the Escherichia coli uridine and thymidine phosphorylases. Unlike widely studied nucleoside analogues, this compound binds to the enzymes irreversibly. Its LD50 in mice was 40 mg/kg. Due to the involvement of pyrimidine phosphorylases in carcinogenesis and the relatively low toxicity of CA-423, it is promising for anticancer therapy.
- Published
- 1998