About: 6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents     Goto   Sponge   NotDistinct   Permalink

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Description
  • Title 6-alkyl-, 6-aryl- and 6-hetaryl-7-deazapurine ribonucleosides previously known as nanomolar cytostatics were found to be potent inhibitors of either human or mycobacterial (MTB) adenosine kinase (ADK). Several new derivatives bearing bulky substituents at position 6 were non-cytotoxic but selectively inhibited MTB ADK. However, most of the nucleosides (ADK inhibitors) as well as their octadecylphosphate prodrugs were inactive in the whole cell assay of inhibition of Mycobacterium bovis growth. 6-Methyl-7-deazapurine ribonucleoside was found to be a potent antimycobacterial agent.
  • Title 6-alkyl-, 6-aryl- and 6-hetaryl-7-deazapurine ribonucleosides previously known as nanomolar cytostatics were found to be potent inhibitors of either human or mycobacterial (MTB) adenosine kinase (ADK). Several new derivatives bearing bulky substituents at position 6 were non-cytotoxic but selectively inhibited MTB ADK. However, most of the nucleosides (ADK inhibitors) as well as their octadecylphosphate prodrugs were inactive in the whole cell assay of inhibition of Mycobacterium bovis growth. 6-Methyl-7-deazapurine ribonucleoside was found to be a potent antimycobacterial agent. (en)
Title
  • 6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents
  • 6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents (en)
skos:prefLabel
  • 6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents
  • 6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents (en)
skos:notation
  • RIV/00216208:11310/13:10193151!RIV14-MSM-11310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • I, P(ED0030/01/01), P(GAP207/11/0344)
http://linked.open...iv/cisloPeriodika
  • 11
http://linked.open...vai/riv/dodaniDat
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  • 119932
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  • RIV/00216208:11310/13:10193151
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  • moiety; discovery; derivatives; purine; crystal-structures; nucleoside analogs; antiseizure activity; 6-(het)aryl-7-deazapurine ribonucleosides; enzyme-inhibition; mycobacterium-tuberculosis (en)
http://linked.open.../riv/klicoveSlovo
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  • US - Spojené státy americké
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  • [830A7CA356B4]
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  • MedChemComm
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  • 4
http://linked.open...iv/tvurceVysledku
  • Džubák, Petr
  • Hocek, Michal
  • Konečný, Petr
  • Pichová, Iva
  • Votruba, Ivan
  • Hajdúch, Marian
  • Perlíková, Pavla
  • Nauš, Petr
  • Snášel, Jan
http://linked.open...ain/vavai/riv/wos
  • 000326244600011
issn
  • 2040-2503
number of pages
http://bibframe.org/vocab/doi
  • 10.1039/c3md00232b
http://localhost/t...ganizacniJednotka
  • 11310
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