About: Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase     Goto   Sponge   NotDistinct   Permalink

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  • Structurally diverse, sugar-modified, thymine-containing nucleoside phosphonic acids were evaluated for their ability to inhibit thymidine phosphorylase purified from spontaneous T-cell lymphomas of an inbred Sprague-Dawley rat strain. From a large set of tested compounds, among them a number of pyrrolidine-based derivatives, 10 nucleotide analogues with IC50 values below 1 .mu.M were selected. Out of them, four compounds strongly inhibited the enzyme with IC50 values in a range of 11–45 nM. These most potent compounds might be bi-substrate analogues.
  • Structurally diverse, sugar-modified, thymine-containing nucleoside phosphonic acids were evaluated for their ability to inhibit thymidine phosphorylase purified from spontaneous T-cell lymphomas of an inbred Sprague-Dawley rat strain. From a large set of tested compounds, among them a number of pyrrolidine-based derivatives, 10 nucleotide analogues with IC50 values below 1 .mu.M were selected. Out of them, four compounds strongly inhibited the enzyme with IC50 values in a range of 11–45 nM. These most potent compounds might be bi-substrate analogues. (en)
Title
  • Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase
  • Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase (en)
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  • Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase
  • Structural diversity of nucleoside phosphonic acids as a key factor in the discovery of potent inhibitors of rat T-cell lymphoma thymidine phosphorylase (en)
skos:notation
  • RIV/61388963:_____/10:00345860!RIV11-GA0-61388963
http://linked.open...avai/riv/aktivita
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  • P(1QS400550501), P(2B06065), P(GA202/09/0193), P(GA203/09/0820), P(KAN200520801), P(LC06061), P(LC06077), P(NR9138), Z(AV0Z40550506)
http://linked.open...iv/cisloPeriodika
  • 3
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 290435
http://linked.open...ai/riv/idVysledku
  • RIV/61388963:_____/10:00345860
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  • phosphonate nucleotides; pyrrolidine; thymidine phosphorylase (en)
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http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [98036BCFC18F]
http://linked.open...i/riv/nazevZdroje
  • Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor
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  • 20
http://linked.open...iv/tvurceVysledku
  • Buděšínský, Miloš
  • Petrová, Magdalena
  • Pohl, Radek
  • Rosenberg, Ivan
  • Votruba, Ivan
  • Vaněk, Václav
  • Rejman, Dominik
  • Králíková, Šárka
  • Panova, Natalya
  • Páv, Ondřej
  • Točík, Zdeněk
  • Liboska, Radek
  • Kočalka, Petr
  • Rinnová, Markéta
  • Tomečková, Ivana
http://linked.open...ain/vavai/riv/wos
  • 000273783800014
http://linked.open...n/vavai/riv/zamer
issn
  • 0960-894X
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