About: Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase

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About: Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	A series of new monophosphates of 1-[2-(phosphonomethoxy)alkyl]thymines, such as PMPTp, 3-MeO-PMPTp, HPMPTp, and FPMPTp, were synthesized, and tested for their ability to inhibit human thymidine phosphorylase. Kinetic measurements of enzyme activity were performed using thymidine and inorganic phosphate as the substrates. The data show that some monophosphates provide a. considerable increase of the multisubstrate inhibitory effect. The highest inhibitory potency was found with (R)-FPMPTp 4c (K-i(dT) = 4.09 +/- 0.47 mu M, K-i(P-i)= 2.13 +/- 0.29 mu M) and (R) 3-MeO-PMPTp 4d (K-i(dT) = 5.78 +/- 0.71 mu M, K-i(P-i)= 2.71 +/- 0.37 mu M). A series of new monophosphates of 1-[2-(phosphonomethoxy)alkyl]thymines, such as PMPTp, 3-MeO-PMPTp, HPMPTp, and FPMPTp, were synthesized, and tested for their ability to inhibit human thymidine phosphorylase. Kinetic measurements of enzyme activity were performed using thymidine and inorganic phosphate as the substrates. The data show that some monophosphates provide a. considerable increase of the multisubstrate inhibitory effect. The highest inhibitory potency was found with (R)-FPMPTp 4c (K-i(dT) = 4.09 +/- 0.47 mu M, K-i(P-i)= 2.13 +/- 0.29 mu M) and (R) 3-MeO-PMPTp 4d (K-i(dT) = 5.78 +/- 0.71 mu M, K-i(P-i)= 2.71 +/- 0.37 mu M). (en)
Title	Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase (en)
skos:prefLabel	Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase Syntheses of 1-[2-(Phosphonomethoxy)Alkyl]Thymine Monophosphates and an Evaluation of their Inhibitory Activity Toward Human Thymidine Phosphorylase (en)
skos:notation	RIV/61388963:_____/12:00376556!RIV13-AV0-61388963
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(1M0508), Z(AV0Z40550506)
http://linked.open...iv/cisloPeriodika	1/3
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Pomeisl, Karel Horská, Květoslava Krečmerová, Marcela Pohl, Radek Blažek, Jiří
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	172906
http://linked.open...ai/riv/idVysledku	RIV/61388963:_____/12:00376556
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	thymidine phosphorylase; phosphorylation; acyclic nucleoside phosphonates (en)
http://linked.open.../riv/klicoveSlovo	acyclic nucleoside phosphonates phosphorylation thymidine phosphorylase
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[6C3E31EC27F3]
http://linked.open...i/riv/nazevZdroje	Nucleosides Nucleotides & Nucleic Acids
http://linked.open...in/vavai/riv/obor	CC
http://linked.open...ichTvurcuVysledku	5 (xsd:int)
http://linked.open...cetTvurcuVysledku	5 (xsd:int)
http://linked.open...vavai/riv/projekt	New Antivirals and Antineoplastics
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	31
http://linked.open...iv/tvurceVysledku	Krečmerová, Marcela Pohl, Radek Blažek, Jiří Horská, Květoslava Pomeisl, Karel
http://linked.open...ain/vavai/riv/wos	000302276700014
http://linked.open...n/vavai/riv/zamer	Regulace biologických procesů: Chemické modulátory vybraných systémů významných pro medicínu a zemědělství
issn	1525-7770
number of pages	13 (xsd:int)
http://bibframe.org/vocab/doi	10.1080/15257770.2011.648361

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