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Bioorg Khim ; 24(12): 920-5, 1998 Dec.
Article in Russian | MEDLINE | ID: mdl-10079951

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.


Subject(s)
Enzyme Inhibitors/pharmacology , Organophosphorus Compounds/pharmacology , Propionates/pharmacology , Thymidine Phosphorylase/antagonists & inhibitors , 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
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