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Statements

Subject Item
n2:RIV%2F61388963%3A_____%2F11%3A00364270%21RIV12-AV0-61388963
rdf:type
skos:Concept n6:Vysledek
dcterms:description
A series of 7-aryl- and 7-hetaryl-7-deazaadenosines were prepared by the cross-coupling reactions of unprotected or protected 7-iodo-7-deazaadenosines with (het)arylboronic acids, stannanes or zinc halides. Nucleosides bearing 5-membered heterocycles at the position 7 exerted potent in vitro anti-proliferative effects against a broad panel of hematological and solid tumor cell lines. Cell cycle analysis indicated profound inhibition of RNA synthesis and induction of apoptosis in treated cells. Intracellular conversion to triphosphates has been detected with active compounds. The triphosphate metabolites showed only a weak inhibitory effect on human RNA polymerase II, suggesting potentially other mechanisms for the inhibition of RNA synthesis and quick onset of apoptosis. Initial in vivo evaluation demonstrated an effect of 7-(2-thienyl)-7-deazaadenine ribonucleoside on the survival rate in syngeneic P388D1 mouse leukemia model. A series of 7-aryl- and 7-hetaryl-7-deazaadenosines were prepared by the cross-coupling reactions of unprotected or protected 7-iodo-7-deazaadenosines with (het)arylboronic acids, stannanes or zinc halides. Nucleosides bearing 5-membered heterocycles at the position 7 exerted potent in vitro anti-proliferative effects against a broad panel of hematological and solid tumor cell lines. Cell cycle analysis indicated profound inhibition of RNA synthesis and induction of apoptosis in treated cells. Intracellular conversion to triphosphates has been detected with active compounds. The triphosphate metabolites showed only a weak inhibitory effect on human RNA polymerase II, suggesting potentially other mechanisms for the inhibition of RNA synthesis and quick onset of apoptosis. Initial in vivo evaluation demonstrated an effect of 7-(2-thienyl)-7-deazaadenine ribonucleoside on the survival rate in syngeneic P388D1 mouse leukemia model.
dcterms:title
Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines
skos:prefLabel
Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines
skos:notation
RIV/61388963:_____/11:00364270!RIV12-AV0-61388963
n6:predkladatel
n7:ico%3A61388963
n3:aktivita
n12:Z n12:S n12:P
n3:aktivity
P(1M0508), P(ED0030/01/01), P(GAP207/11/0344), P(LC07017), S, Z(AV0Z40550506)
n3:cisloPeriodika
15
n3:dodaniDat
n11:2012
n3:domaciTvurceVysledku
n4:3603652 n4:8571325 n4:1703404 n4:8555346 n4:2264102 n4:6659160 Bourderioux, Aurelie
n3:druhVysledku
n18:J
n3:duvernostUdaju
n15:S
n3:entitaPredkladatele
n13:predkladatel
n3:idSjednocenehoVysledku
233881
n3:idVysledku
RIV/61388963:_____/11:00364270
n3:jazykVysledku
n20:eng
n3:klicovaSlova
adenosine-kinase-inhibitors; cross-coupling reactions; cytotoxic nucleoside analogs; enzyme-inhibition; ribonucleosides
n3:klicoveSlovo
n14:cytotoxic%20nucleoside%20analogs n14:adenosine-kinase-inhibitors n14:enzyme-inhibition n14:ribonucleosides n14:cross-coupling%20reactions
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[0D61CD2AFD07]
n3:nazevZdroje
Journal of Medicinal Chemistry
n3:obor
n16:CC
n3:pocetDomacichTvurcuVysledku
7
n3:pocetTvurcuVysledku
16
n3:projekt
n9:ED0030%2F01%2F01 n9:GAP207%2F11%2F0344 n9:LC07017 n9:1M0508
n3:rokUplatneniVysledku
n11:2011
n3:svazekPeriodika
54
n3:tvurceVysledku
Perlíková, Pavla Votruba, Ivan Birkuš, G. Wang, T. Bourderioux, Aurelie Stray, K. M. Nauš, Petr Cihlar, T. Pohl, Radek Konečný, P. Feng, J. Y. Džubák, P. Hocek, Michal Hajdúch, M. Ray, A. S. Pichová, Iva
n3:wos
000293419400021
n3:zamer
n17:AV0Z40550506
s:issn
0022-2623
s:numberOfPages
10
n19:doi
10.1021/jm2005173