About: Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
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. (en)
Title	Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines (en)
skos:prefLabel	Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines Synthesis and Significant Cytostatic Activity of 7-Hetaryl-7-deazaadenosines (en)
skos:notation	RIV/61388963:_____/11:00364270!RIV12-AV0-61388963
http://linked.open...avai/riv/aktivita	P S Z
http://linked.open...avai/riv/aktivity	P(1M0508), P(ED0030/01/01), P(GAP207/11/0344), P(LC07017), S, Z(AV0Z40550506)
http://linked.open...iv/cisloPeriodika	15
http://linked.open...vai/riv/dodaniDat	2012
http://linked.open...aciTvurceVysledku	Votruba, Ivan Pichová, Iva Pohl, Radek Hocek, Michal Perlíková, Pavla Nauš, Petr Bourderioux, Aurelie
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	233881
http://linked.open...ai/riv/idVysledku	RIV/61388963:_____/11:00364270
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	adenosine-kinase-inhibitors; cross-coupling reactions; cytotoxic nucleoside analogs; enzyme-inhibition; ribonucleosides (en)
http://linked.open.../riv/klicoveSlovo	adenosine-kinase-inhibitors cross-coupling reactions cytotoxic nucleoside analogs enzyme-inhibition ribonucleosides
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[0D61CD2AFD07]
http://linked.open...i/riv/nazevZdroje	Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CC
http://linked.open...ichTvurcuVysledku	7 (xsd:int)
http://linked.open...cetTvurcuVysledku	16 (xsd:int)
http://linked.open...vavai/riv/projekt	New Antivirals and Antineoplastics Biomedicine for regional development and human resources Oncoproteomics Centre Combinatorial and rational approaches for the synthesis and evaluation of novel modified nucleosides with cytostatic and antimicrobial activity
http://linked.open...UplatneniVysledku	2011
http://linked.open...v/svazekPeriodika	54
http://linked.open...iv/tvurceVysledku	Cihlar, T. Hocek, Michal Konečný, P. Pichová, Iva Pohl, Radek Votruba, Ivan Birkuš, G. Perlíková, Pavla Bourderioux, Aurelie Džubák, P. Feng, J. Y. Hajdúch, M. Nauš, Petr Ray, A. S. Stray, K. M. Wang, T.
http://linked.open...ain/vavai/riv/wos	000293419400021
http://linked.open...n/vavai/riv/zamer	Regulace biologických procesů: Chemické modulátory vybraných systémů významných pro medicínu a zemědělství
issn	0022-2623
number of pages	10 (xsd:int)
http://bibframe.org/vocab/doi	10.1021/jm2005173

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