About: Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Roscovitine is a synthetic inhibitor of cyclin-dependent kinases that is currently undergoing clinical trials as a candidate drug for some oncological indications. Its discovery prompted many research teams to further optimize its structure or to initiate their own related but independent studies. This article reviews known roscovitine bioisosteres that have been prepared as CDK inhibitors using different core heterocycles. The individual bioisostere types have been described and explored to a different extent, which complicates direct comparisons of their biochemical activity - only six direct analogs containing different purine bioisosteres have been prepared and evaluated side by side with roscovitine. Only four types of bioisosteres have demonstrated improved biological properties, namely pyrazolo[1,5-a]-1,3,5-triazines, pyrazolo[1,5-a]pyrimidines, pyrazolo[1,5-a]pyridines and pyrazolo[4,3-d] pyrimidines. Roscovitine is a synthetic inhibitor of cyclin-dependent kinases that is currently undergoing clinical trials as a candidate drug for some oncological indications. Its discovery prompted many research teams to further optimize its structure or to initiate their own related but independent studies. This article reviews known roscovitine bioisosteres that have been prepared as CDK inhibitors using different core heterocycles. The individual bioisostere types have been described and explored to a different extent, which complicates direct comparisons of their biochemical activity - only six direct analogs containing different purine bioisosteres have been prepared and evaluated side by side with roscovitine. Only four types of bioisosteres have demonstrated improved biological properties, namely pyrazolo[1,5-a]-1,3,5-triazines, pyrazolo[1,5-a]pyrimidines, pyrazolo[1,5-a]pyridines and pyrazolo[4,3-d] pyrimidines. (en)
Title	Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres (en)
skos:prefLabel	Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres (en)
skos:notation	RIV/61989592:15310/12:33142792!RIV13-MSM-15310___
http://linked.open...avai/predkladatel	Přírodovědecká fakulta
http://linked.open...avai/riv/aktivita	P R Z
http://linked.open...avai/riv/aktivity	P(ED1.100/02/0123), P(GA301/08/1649), P(GAP305/12/0783), R, Z(AV0Z50380511), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika	20
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Jorda, Radek Kryštof, Vladimír Paruch, Kamil
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	129350
http://linked.open...ai/riv/idVysledku	RIV/61989592:15310/12:33142792
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	bioisostere; roscovitine; inhibitor; cyclin-dependent kinase; Cancer (en)
http://linked.open.../riv/klicoveSlovo	Cancer bioisostere cyclin-dependent kinase roscovitine inhibitor
http://linked.open...odStatuVydavatele	NL - Nizozemsko
http://linked.open...ontrolniKodProRIV	[55503299E347]
http://linked.open...i/riv/nazevZdroje	Current Pharmaceutical Design
http://linked.open...in/vavai/riv/obor	ED
http://linked.open...ichTvurcuVysledku	3 (xsd:int)
http://linked.open...cetTvurcuVysledku	3 (xsd:int)
http://linked.open...vavai/riv/projekt	Evaluation of cyclin-dependent kinase inhibitors in cancer cell lines with specific genetic alterations Modulation of cell division of normal and cancer cells by cyclin-dependent kinase inhibitors St. Anne´s University Hospital Brno - International Clinical Research Center (FNUSA-ICRC)
http://linked.open...UplatneniVysledku	2012
http://linked.open...v/svazekPeriodika	18
http://linked.open...iv/tvurceVysledku	Jorda, Radek Kryštof, Vladimír Paruch, Kamil
http://linked.open...ain/vavai/riv/wos	000306547500013
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 Modulation of signalling and regulatory pathways in normal and cancer cells
issn	1381-6128
number of pages	7 (xsd:int)
http://localhost/t...ganizacniJednotka	15310
is http://linked.open...avai/riv/vysledek of	Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres

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