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Statements

Subject Item
n2:RIV%2F00216208%3A11310%2F13%3A10193151%21RIV14-MSM-11310___
rdf:type
n6:Vysledek skos:Concept
rdfs:seeAlso
http://dx.doi.org/10.1039/c3md00232b
dcterms: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.
dcterms: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
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
skos:notation
RIV/00216208:11310/13:10193151!RIV14-MSM-11310___
n6:predkladatel
n11:orjk%3A11310
n3:aktivita
n21:P n21:I
n3:aktivity
I, P(ED0030/01/01), P(GAP207/11/0344)
n3:cisloPeriodika
11
n3:dodaniDat
n4:2014
n3:domaciTvurceVysledku
n20:6659160
n3:druhVysledku
n18:J
n3:duvernostUdaju
n14:S
n3:entitaPredkladatele
n15:predkladatel
n3:idSjednocenehoVysledku
119932
n3:idVysledku
RIV/00216208:11310/13:10193151
n3:jazykVysledku
n10:eng
n3:klicovaSlova
moiety; discovery; derivatives; purine; crystal-structures; nucleoside analogs; antiseizure activity; 6-(het)aryl-7-deazapurine ribonucleosides; enzyme-inhibition; mycobacterium-tuberculosis
n3:klicoveSlovo
n8:derivatives n8:mycobacterium-tuberculosis n8:crystal-structures n8:enzyme-inhibition n8:discovery n8:purine n8:nucleoside%20analogs n8:6-%28het%29aryl-7-deazapurine%20ribonucleosides n8:moiety n8:antiseizure%20activity
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[830A7CA356B4]
n3:nazevZdroje
MedChemComm
n3:obor
n13:CC
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
9
n3:projekt
n5:ED0030%2F01%2F01 n5:GAP207%2F11%2F0344
n3:rokUplatneniVysledku
n4:2013
n3:svazekPeriodika
4
n3:tvurceVysledku
Hajdúch, Marian Džubák, Petr Pichová, Iva Perlíková, Pavla Votruba, Ivan Nauš, Petr Snášel, Jan Hocek, Michal Konečný, Petr
n3:wos
000326244600011
s:issn
2040-2503
s:numberOfPages
4
n16:doi
10.1039/c3md00232b
n19:organizacniJednotka
11310