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rdf:type
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Description
| - A series of conformationally constrained uridine-based nucleoside phosphonic acids containing annealed 1,3-dioxolane and 1,4-dioxane rings and their %22open-structure%22 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 K-i values in the range of 0.048-1 mu M. The inhibition potency of the studied compounds strongly depended on the degree of conformational flexibility of the phosphonate moiety, the stereochemical arrangement of the sugarphosphonate component, and the substituent at position 5 of the pyrimidine nucleobase.
- A series of conformationally constrained uridine-based nucleoside phosphonic acids containing annealed 1,3-dioxolane and 1,4-dioxane rings and their %22open-structure%22 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 K-i values in the range of 0.048-1 mu M. The inhibition potency of the studied compounds strongly depended on the degree of conformational flexibility of the phosphonate moiety, the stereochemical arrangement of the sugarphosphonate component, and the substituent at position 5 of the pyrimidine nucleobase. (en)
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Title
| - Inhibition of human thymidine phosphorylase by conformationally constrained pyrimidine nucleoside phosphonic acids and their %22open-structure%22 isosteres
- Inhibition of human thymidine phosphorylase by conformationally constrained pyrimidine nucleoside phosphonic acids and their %22open-structure%22 isosteres (en)
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skos:prefLabel
| - Inhibition of human thymidine phosphorylase by conformationally constrained pyrimidine nucleoside phosphonic acids and their %22open-structure%22 isosteres
- Inhibition of human thymidine phosphorylase by conformationally constrained pyrimidine nucleoside phosphonic acids and their %22open-structure%22 isosteres (en)
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skos:notation
| - RIV/61388963:_____/14:00428628!RIV15-GA0-61388963
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
| - I, P(GA13-24880S), P(GA13-26526S), P(GA202/09/0193), P(GA203/09/0820)
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/61388963:_____/14:00428628
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - phosphonate; conformationally constrained nucleotide analog; human thymidine phosphorylase; PBMC; bi-substrate-like inhibitor; Michael addition (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - FR - Francouzská republika
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - European Journal of Medicinal Chemistry
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Buděšínský, Miloš
- Petrová, Magdalena
- Rosenberg, Ivan
- Šimák, Ondřej
- Rejman, Dominik
- Kóšiová, Ivana
- Panova, Natalya
- Páv, Ondřej
- Liboska, Radek
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http://linked.open...ain/vavai/riv/wos
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issn
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number of pages
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http://bibframe.org/vocab/doi
| - 10.1016/j.ejmech.2013.12.026
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