About: New heterocyclic compounds with strong CDK inhibitory and anticancer properties.     Goto   Sponge   NotDistinct   Permalink

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  • 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.
  • 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. (en)
  • 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. (cs)
Title
  • New heterocyclic compounds with strong CDK inhibitory and anticancer properties.
  • New heterocyclic compounds with strong CDK inhibitory and anticancer properties. (en)
  • Nové heterocyklické sloučeniny se silnými CDK-inhibičními a protinádorovými vlastnostmi. (cs)
skos:prefLabel
  • New heterocyclic compounds with strong CDK inhibitory and anticancer properties.
  • New heterocyclic compounds with strong CDK inhibitory and anticancer properties. (en)
  • Nové heterocyklické sloučeniny se silnými CDK-inhibičními a protinádorovými vlastnostmi. (cs)
skos:notation
  • RIV/61989592:15310/04:00002120!RIV/2005/MSM/153105/N
http://linked.open.../vavai/riv/strany
  • B6
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • Z(MSM 153100008)
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 576090
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15310/04:00002120
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • CDK;purine inhibitors;cell cycle (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...ontrolniKodProRIV
  • [7F59BE0FBBC5]
http://linked.open...i/riv/mistoVydani
  • Florida
http://linked.open...i/riv/nazevZdroje
  • Cell Cycle and Cancer: Pathways and Therapies
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...iv/tvurceVysledku
  • Havlíček, Libor
  • Kryštof, Vladimír
  • Strnad, Miroslav
  • Lenobel, René
http://linked.open...n/vavai/riv/zamer
number of pages
http://purl.org/ne...btex#hasPublisher
  • American Association for Cancer Research
http://localhost/t...ganizacniJednotka
  • 15310
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