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