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[A new inhibitor of pyrimidine phosphorylase].
- Source :
-
Bioorganicheskaia khimiia [Bioorg Khim] 1998 Dec; Vol. 24 (12), pp. 920-5. - Publication Year :
- 1998
-
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.
- 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
Subjects
Details
- Language :
- Russian
- ISSN :
- 0132-3423
- Volume :
- 24
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganicheskaia khimiia
- Publication Type :
- Academic Journal
- Accession number :
- 10079951