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Inhibition of human thymidine phosphorylase by conformationally constrained pyrimidine nucleoside phosphonic acids and their "open-structure" isosteres
I. Košiová, O. Šimák, N. Panova, M. Buděšínský, M. Petrová, D. Rejman, R. Liboska, O. Páv, I. Rosenberg,
Jazyk angličtina Země Francie
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- inhibitory enzymů farmakologie MeSH
- kyseliny fosforité chemie farmakologie MeSH
- lidé MeSH
- molekulární konformace MeSH
- pyrimidinové nukleosidy farmakologie MeSH
- thymidinfosforylasa antagonisté a inhibitory MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
A series of conformationally constrained uridine-based nucleoside phosphonic acids containing annealed 1,3-dioxolane and 1,4-dioxane rings and their "open-structure" isosteres were synthesized and evaluated as potential multisubstrate-like inhibitors of the human recombinant thymidine phosphorylase (TP, EC 2.4.2.4) and TP obtained from peripheral blood mononuclear cells (PBMC). From a large set of tested nucleoside phosphonic acids, several potent compounds were identified that exhibited Ki values in the range of 0.048-1 μM. The inhibition potency of the studied compounds strongly depended on the degree of conformational flexibility of the phosphonate moiety, the stereochemical arrangement of the sugar-phosphonate component, and the substituent at position 5 of the pyrimidine nucleobase.
Citace poskytuje Crossref.org
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