About: Inhibition of human thymidine phosphorylase by conformationally constrained pyrimidine nucleoside phosphonic acids and their %22open-structure%22 isosteres

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About: Inhibition of human thymidine phosphorylase by conformationally constrained pyrimidine nucleoside phosphonic acids and their %22open-structure%22 isosteres Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
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)
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)
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)
skos:notation	RIV/61388963:_____/14:00428628!RIV15-GA0-61388963
http://linked.open...avai/riv/aktivita	I P
http://linked.open...avai/riv/aktivity	I, P(GA13-24880S), P(GA13-26526S), P(GA202/09/0193), P(GA203/09/0820)
http://linked.open...iv/cisloPeriodika	Mar 3
http://linked.open...vai/riv/dodaniDat	2015
http://linked.open...aciTvurceVysledku	Rosenberg, Ivan Petrová, Magdalena Buděšínský, Miloš Rejman, Dominik Kóšiová, Ivana Páv, Ondřej Liboska, Radek Šimák, Ondřej Panova, Natalya
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav organické chemie a biochemie AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	21847
http://linked.open...ai/riv/idVysledku	RIV/61388963:_____/14:00428628
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	phosphonate; conformationally constrained nucleotide analog; human thymidine phosphorylase; PBMC; bi-substrate-like inhibitor; Michael addition (en)
http://linked.open.../riv/klicoveSlovo	Michael addition PBMC bi-substrate-like inhibitor conformationally constrained nucleotide analog human thymidine phosphorylase phosphonate
http://linked.open...odStatuVydavatele	FR - Francouzská republika
http://linked.open...ontrolniKodProRIV	[285C1FE5E6BE]
http://linked.open...i/riv/nazevZdroje	European Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CC
http://linked.open...ichTvurcuVysledku	9 (xsd:int)
http://linked.open...cetTvurcuVysledku	9 (xsd:int)
http://linked.open...vavai/riv/projekt	Nové DNA a RNA oligonukleotidy s fosfonothioátovými a fosfonoamidátovými internukleotidovými vazbami Struktura a vlastnosti modifikovaných složek nukleových kyselin Formation and dynamics of nucleic acid motifs involved in regulation of gene expression Structure based drug design of specific nucleotidases inhibitors, potentially pharmacologically important compounds.
http://linked.open...UplatneniVysledku	2014
http://linked.open...v/svazekPeriodika	74
http://linked.open...iv/tvurceVysledku	Buděšínský, Miloš Petrová, Magdalena Rosenberg, Ivan Šimák, Ondřej Rejman, Dominik Kóšiová, Ivana Panova, Natalya Páv, Ondřej Liboska, Radek
http://linked.open...ain/vavai/riv/wos	000333780800015
issn	0223-5234
number of pages	24 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.ejmech.2013.12.026

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