About: A Novel Series of Highly Potent 2,6,9-Trisubstituted Purine Cyclin-Dependent Kinase Inhibitors

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About: A Novel Series of Highly Potent 2,6,9-Trisubstituted Purine Cyclin-Dependent Kinase Inhibitors Goto Sponge NotDistinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	The inhibition of overactive CDKs during cancer remains an important strategy in cancer drug development. We synthesized and screened a novel series of 2-substituted-6-biarylmethylamino-9-cyclopentylpurine derivatives for improved CDK inhibitory activity and antiproliferative effects. One of the most potent compounds, 6b, exhibited strong cytotoxicity in the human melanoma cell line G361 that correlated with robust CDK1 and CDK2 inhibition and caspase activation. In silico modeling of 6b in the active site of CDK2 revealed a high interaction energy, which we believe is due to the 6-heterobiarylmethylamino substitution of the purine moiety. The inhibition of overactive CDKs during cancer remains an important strategy in cancer drug development. We synthesized and screened a novel series of 2-substituted-6-biarylmethylamino-9-cyclopentylpurine derivatives for improved CDK inhibitory activity and antiproliferative effects. One of the most potent compounds, 6b, exhibited strong cytotoxicity in the human melanoma cell line G361 that correlated with robust CDK1 and CDK2 inhibition and caspase activation. In silico modeling of 6b in the active site of CDK2 revealed a high interaction energy, which we believe is due to the 6-heterobiarylmethylamino substitution of the purine moiety. (en)
Title	A Novel Series of Highly Potent 2,6,9-Trisubstituted Purine Cyclin-Dependent Kinase Inhibitors A Novel Series of Highly Potent 2,6,9-Trisubstituted Purine Cyclin-Dependent Kinase Inhibitors (en)
skos:prefLabel	A Novel Series of Highly Potent 2,6,9-Trisubstituted Purine Cyclin-Dependent Kinase Inhibitors A Novel Series of Highly Potent 2,6,9-Trisubstituted Purine Cyclin-Dependent Kinase Inhibitors (en)
skos:notation	RIV/61389030:_____/13:00399222!RIV14-GA0-61389030
http://linked.open...avai/riv/aktivita	P S Z
http://linked.open...avai/riv/aktivity	P(ED0007/01/01), P(ED2.1.00/03.0058), P(EE2.3.20.0017), P(GAP305/12/0783), P(GD203/09/H046), S, Z(AV0Z50380511)
http://linked.open...iv/cisloPeriodika	15
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Jorda, Radek Kryštof, Vladimír Řezníčková, Eva Strnad, Miroslav
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 experimentální botaniky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	58915
http://linked.open...ai/riv/idVysledku	RIV/61389030:_____/13:00399222
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	CHRONIC LYMPHOCYTIC-LEUKEMIA; DINACICLIB SCH 727965; CELL-CYCLE (en)
http://linked.open.../riv/klicoveSlovo	CHRONIC LYMPHOCYTIC-LEUKEMIA DINACICLIB SCH 727965 CELL-CYCLE
http://linked.open...odStatuVydavatele	US - Spojené státy americké
http://linked.open...ontrolniKodProRIV	[0C30A789AD2A]
http://linked.open...i/riv/nazevZdroje	Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	ED
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	9 (xsd:int)
http://linked.open...vavai/riv/projekt	Regional Centre of Advanced Technologies and Materials Research team development of the Regional Centre of Advanced Technologies and Materials Evaluation of cyclin-dependent kinase inhibitors in cancer cell lines with specific genetic alterations Centre of the Region Haná for Biotechnological and Agricultural Research Biochemistry on the crossroad from in silico to in vitro
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	56
http://linked.open...iv/tvurceVysledku	Jorda, Radek Kryštof, Vladimír Strnad, Miroslav Zatloukal, M. Bazgier, V. Berka, K. Béres, T. Gucký, T. Řezníčková, Eva
http://linked.open...ain/vavai/riv/wos	000323082400018
http://linked.open...n/vavai/riv/zamer	Mechanismy regulace růstu a vývoje rostlin na úrovni buněk, orgánů a celých organismů: fyziologické, genetické a molekulárně biologické základy
issn	0022-2623
number of pages	14 (xsd:int)
http://bibframe.org/vocab/doi	10.1021/jm4006884

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