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Statements

Subject Item
n2:RIV%2F61989592%3A15310%2F04%3A00002120%21RIV%2F2005%2FMSM%2F153105%2FN
rdf:type
n15:Vysledek skos:Concept
dcterms:description
Recently, a deregulation of cyclin-dependent kinases (CDKs) has been proved in human primary tumors and in tumor cell lines. The discovery evoked a strong interest in inhibitors of CDKs that could play a role in the therapy of cancers. Series of 2-, 6-, 8-, 9-tetrasubstituted purines, 3-, 7-disubstituted pyrazolo 4,3-d pyrimidines, and 2-, 6-, 9-trisubstituted 1,2,3-triazolo 4,5-d pyrimidines (8-azapurines), which specifically inhibits some CDKs at micromolar concentrations have been developed.. The compounds display (1) an enhanced inhibitory activity toward CDK1/2, or (2) a higher selectivity for some CDKs, or (3) an increased antimitotic activity at the G1/S and G2/M points of the cell cycle, and finally (4) stronger and more selective antitumor effects. Hence they can be used as antimitotic drugs, in particular, in chemotherapy of cancer, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer´s disease or as antineurodegenerative drugs. Deregulace cyklin-dependentních (CDK) kinas úzce souvisí se vznikem růstem nádorů. Tato skutečnost vyvolala zájem o specifické inhibitory CDK použitelné v terapii nádorových onemocnění. Vyvinuli jsme série specifických inhibitorů CDK na bázi 2,6,8,9-tetrasubstituovaných purinů, 3,7-disubstituovaných pyrazolo[4,3-d]pyrimidinů a 2,6,9-trisubstituovaných 1,2,3-triazolo[4,5-d]pyrimidinů (8-azapurinů). Tyto sloučeniny vykazují silnou inhibiční aktivitu na CDK1/2, vyšší selektivitu pro CDK, silnou antimitotickou aktivitu a pozoruhodné protinádorové účinky. Mohou proto být použity jako antimitotické látky, zvláště pak jako protinádorová chemoterapeutika, léčiva pro prosiasu, parasitosy, Alzeimerovy choroby a jiných antineurodegenerativních poruch. Recently, a deregulation of cyclin-dependent kinases (CDKs) has been proved in human primary tumors and in tumor cell lines. The discovery evoked a strong interest in inhibitors of CDKs that could play a role in the therapy of cancers. Series of 2-, 6-, 8-, 9-tetrasubstituted purines, 3-, 7-disubstituted pyrazolo 4,3-d pyrimidines, and 2-, 6-, 9-trisubstituted 1,2,3-triazolo 4,5-d pyrimidines (8-azapurines), which specifically inhibits some CDKs at micromolar concentrations have been developed.. The compounds display (1) an enhanced inhibitory activity toward CDK1/2, or (2) a higher selectivity for some CDKs, or (3) an increased antimitotic activity at the G1/S and G2/M points of the cell cycle, and finally (4) stronger and more selective antitumor effects. Hence they can be used as antimitotic drugs, in particular, in chemotherapy of cancer, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer´s disease or as antineurodegenerative drugs.
dcterms:title
Nové heterocyklické sloučeniny se silnými CDK-inhibičními a protinádorovými vlastnostmi. New heterocyclic compounds with strong CDK inhibitory and anticancer properties. New heterocyclic compounds with strong CDK inhibitory and anticancer properties.
skos:prefLabel
Nové heterocyklické sloučeniny se silnými CDK-inhibičními a protinádorovými vlastnostmi. New heterocyclic compounds with strong CDK inhibitory and anticancer properties. New heterocyclic compounds with strong CDK inhibitory and anticancer properties.
skos:notation
RIV/61989592:15310/04:00002120!RIV/2005/MSM/153105/N
n3:strany
B6
n3:aktivita
n18:Z
n3:aktivity
Z(MSM 153100008)
n3:dodaniDat
n7:2005
n3:domaciTvurceVysledku
n13:9896821 n13:9961216 n13:4712048
n3:druhVysledku
n14:D
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n12:predkladatel
n3:idSjednocenehoVysledku
576090
n3:idVysledku
RIV/61989592:15310/04:00002120
n3:jazykVysledku
n8:eng
n3:klicovaSlova
CDK;purine inhibitors;cell cycle
n3:klicoveSlovo
n5:purine%20inhibitors n5:cell%20cycle n5:CDK
n3:kontrolniKodProRIV
[7F59BE0FBBC5]
n3:mistoVydani
Florida
n3:nazevZdroje
Cell Cycle and Cancer: Pathways and Therapies
n3:obor
n19:ED
n3:pocetDomacichTvurcuVysledku
3
n3:pocetTvurcuVysledku
4
n3:rokUplatneniVysledku
n7:2004
n3:tvurceVysledku
Lenobel, René Strnad, Miroslav Kryštof, Vladimír Havlíček, Libor
n3:zamer
n10:MSM%20153100008
s:numberOfPages
225
n9:hasPublisher
American Association for Cancer Research
n11:organizacniJednotka
15310