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[A new inhibitor of pyrimidine phosphorylase].

Authors :
Dmitrieva NA
Molchan OK
Komissarov AA
Sokolov VB
Aksinenko AIu
Pushin AN
Chekhlov AN
Debabov VG
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.

Details

Language :
Russian
ISSN :
0132-3423
Volume :
24
Issue :
12
Database :
MEDLINE
Journal :
Bioorganicheskaia khimiia
Publication Type :
Academic Journal
Accession number :
10079951