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[A new inhibitor of pyrimidine phosphorylase]. 1998
N A Dmitrieva, and
O K Molchan, and
A A Komissarov, and
V B Sokolov, and
A Iu Aksinenko, and
A N Pushin, and
A N Chekhlov, and
V G Debabov
State Research Institute of Genetics and Selection of Industrial Microorganisms, Moscow, Russia. komissar@vnigen.msk.su
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.
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