About: Tetrasubstituted purines as inhibitors of CDK1

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Cyclin-dependent kinases (CDKs) have raised considerable attention because of their pivotal role in the regulation of cell division cycle. Due to their hyperactivation in a number of transformed cells, drug discovery programs direct the effort towards the identification of chemical inhibitors of CDKs as anticancer agents. In our effort to enhance the affinity of purine inhibitors to CDKs, we introduced another side chain at C8. The straightforward syntheses of 2,6,8,9-tetrasubstituted purines [1-3] generally started from previously synthesised 2,6,9-trisubstituted purines [4,5] and are described in details (see Scheme 1). The inhibitor-CDK mutual interactions between CDK2 and inhibitor were subsequently verified by molecular modelling [6]. The introduced C8 substituents, however, lowered the CDK inhibitory activity, whereas the antiproliferative activity of several derivatives remained high (Tab. 1.). Cyclin-dependent kinases (CDKs) have raised considerable attention because of their pivotal role in the regulation of cell division cycle. Due to their hyperactivation in a number of transformed cells, drug discovery programs direct the effort towards the identification of chemical inhibitors of CDKs as anticancer agents. In our effort to enhance the affinity of purine inhibitors to CDKs, we introduced another side chain at C8. The straightforward syntheses of 2,6,8,9-tetrasubstituted purines [1-3] generally started from previously synthesised 2,6,9-trisubstituted purines [4,5] and are described in details (see Scheme 1). The inhibitor-CDK mutual interactions between CDK2 and inhibitor were subsequently verified by molecular modelling [6]. The introduced C8 substituents, however, lowered the CDK inhibitory activity, whereas the antiproliferative activity of several derivatives remained high (Tab. 1.). (en)
Title	Tetrasubstituted purines as inhibitors of CDK1 Tetrasubstituted purines as inhibitors of CDK1 (en)
skos:prefLabel	Tetrasubstituted purines as inhibitors of CDK1 Tetrasubstituted purines as inhibitors of CDK1 (en)
skos:notation	RIV/61989592:15310/03:00001584!RIV/2004/GA0/153104/N
http://linked.open.../vavai/riv/strany	596
http://linked.open...avai/riv/aktivita	P
http://linked.open...avai/riv/aktivity	P(GA301/02/0475)
http://linked.open...iv/cisloPeriodika	8
http://linked.open...vai/riv/dodaniDat	2004
http://linked.open...aciTvurceVysledku	Kryštof, Vladimír Hanuš, Jan Strnad, Miroslav Otyepka, Michal
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	Univerzita Palackého v Olomouci / Přírodovědecká fakulta
http://linked.open...dnocenehoVysledku	630776
http://linked.open...ai/riv/idVysledku	RIV/61989592:15310/03:00001584
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	purine, inhibitor, CDK1 (en)
http://linked.open.../riv/klicoveSlovo	purine inhibitor CDK1
http://linked.open...odStatuVydavatele	PL - Polská republika
http://linked.open...ontrolniKodProRIV	[3EEF522FB5EA]
http://linked.open...i/riv/nazevZdroje	Cellular & Molecular Biology Letters
http://linked.open...in/vavai/riv/obor	ED
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	8 (xsd:int)
http://linked.open...ocetUcastnikuAkce	0 (xsd:int)
http://linked.open...nichUcastnikuAkce	0 (xsd:int)
http://linked.open...vavai/riv/projekt	Purine inhibitors of cyclin-dependent kinases as anticancer and antimitotic compounds
http://linked.open...UplatneniVysledku	2003
http://linked.open...v/svazekPeriodika	8
http://linked.open...iv/tvurceVysledku	Hanuš, Jan Kryštof, Vladimír Otyepka, Michal Strnad, Miroslav Moravec, J. Fuksová, K. Havlíček, L. Moravcová, D.
issn	1425-8153
number of pages	1 (xsd:int)
http://localhost/t...ganizacniJednotka	15310

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