About: Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Řada N3-substituovaných acyklických nukleosidových fosfonátů nesoucích (fosfonomethoxy)alkylové skupiny byly připraveny a testovány pro jejich schopnost inhibovat lidskou thymidinfosforylasu exprimovanou z V79 buňek činských křečků stejně jako vůči thymidinfosforylasám z SD-lymfomu, Escherichia coli a lidské placenty. V porovnání z N1-substituovanými analogy, které mají významnou inhibiční aktivitu vůči thymidinfosforylase z SD-lymfomu, výsledky ukázaly nedostatečný inhibiční efekt těchto sloučenin. Žádný z prezentovaných N3-substituovaných derivátů nemá významnou cytostatickou aktivitu. (cs) A series of N3-substituted thymine acyclic nucleoside phosphonates bearing a number of (phosphonomethoxy)alkyl groups were synthesized and investigated for their ability to inhibit the human thymidine phosphorylase expressed in V79 Chinese hamster cells, as well as thymidine phosphorylase from SD-lymphoma, Escherichia coli and human placenta. In comparison to N1- substituted analogues which possess a considerable inhibitory activity towards thymidine phosphorylase from SD-lymphoma, the results showed a marginal inhibitory effect of these compounds. None of the presented N3-substituted derivatives possess a significant cytostatic activity. A series of N3-substituted thymine acyclic nucleoside phosphonates bearing a number of (phosphonomethoxy)alkyl groups were synthesized and investigated for their ability to inhibit the human thymidine phosphorylase expressed in V79 Chinese hamster cells, as well as thymidine phosphorylase from SD-lymphoma, Escherichia coli and human placenta. In comparison to N1- substituted analogues which possess a considerable inhibitory activity towards thymidine phosphorylase from SD-lymphoma, the results showed a marginal inhibitory effect of these compounds. None of the presented N3-substituted derivatives possess a significant cytostatic activity. (en)
Title	Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase (en) Syntézy N3-substituovaných thyminových acyklických nukleosidových fosfonátů a zhodnocení jejich inhibičního účinku vůči thymidinfosforylase (cs)
skos:prefLabel	Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase (en) Syntézy N3-substituovaných thyminových acyklických nukleosidových fosfonátů a zhodnocení jejich inhibičního účinku vůči thymidinfosforylase (cs)
skos:notation	RIV/61388963:_____/08:00305693!RIV08-AV0-61388963
http://linked.open.../vavai/riv/strany	1364;1367
http://linked.open...avai/riv/aktivita	Z
http://linked.open...avai/riv/aktivity	Z(AV0Z40550506)
http://linked.open...iv/cisloPeriodika	4
http://linked.open...vai/riv/dodaniDat	2008
http://linked.open...aciTvurceVysledku	Pomeisl, Karel Votruba, Ivan Holý, Antonín Pohl, Radek
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	398706
http://linked.open...ai/riv/idVysledku	RIV/61388963:_____/08:00305693
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	acyclic nucleoside phosphonates; thymidine phosphorylase; fluorination; pyrimidine (en)
http://linked.open.../riv/klicoveSlovo	fluorination pyrimidine acyclic nucleoside phosphonates thymidine phosphorylase
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[5BFF064B6517]
http://linked.open...i/riv/nazevZdroje	Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	CC
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	4 (xsd:int)
http://linked.open...UplatneniVysledku	2008
http://linked.open...v/svazekPeriodika	18
http://linked.open...iv/tvurceVysledku	Holý, Antonín Pohl, Radek Votruba, Ivan Pomeisl, Karel
http://linked.open...n/vavai/riv/zamer	Regulace biologických procesů: Chemické modulátory vybraných systémů významných pro medicínu a zemědělství
issn	0960-894X
number of pages	4 (xsd:int)
is http://linked.open...avai/riv/vysledek of	Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase Syntheses of N3-substituted thymine acyclic nucleoside phosphonates and a comparison of their inhibitory effect towards thymidine phosphorylase

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