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  • Based on our previous experiences with synthesis of purines, novel 2,6,9-trisubstituted purine derivatives were prepared and assayed for the ability to inhibit CDK1/cyclin B kinase. One of newly synthesized compounds designated as olomoucine II, 6-[(2-hydroxybenzyl)amino]-2-{[1-(hydroxymethyl)propyl]amino}-9-isopropylpurine, displays 10 times higher inhibitory activity than roscovitine, potent and specific CDK1 inhibitor. Olomoucine II in vitro cytotoxic activity exceeds purvalanol A, the most potent CDK inhibitor, as it kills the CEM cells with IC50 value of 3.0 micro M.
  • Based on our previous experiences with synthesis of purines, novel 2,6,9-trisubstituted purine derivatives were prepared and assayed for the ability to inhibit CDK1/cyclin B kinase. One of newly synthesized compounds designated as olomoucine II, 6-[(2-hydroxybenzyl)amino]-2-{[1-(hydroxymethyl)propyl]amino}-9-isopropylpurine, displays 10 times higher inhibitory activity than roscovitine, potent and specific CDK1 inhibitor. Olomoucine II in vitro cytotoxic activity exceeds purvalanol A, the most potent CDK inhibitor, as it kills the CEM cells with IC50 value of 3.0 micro M. (en)
Title
  • Synthesis and biological activity of olomoucine II.
  • Synthesis and biological activity of olomoucine II. (en)
skos:prefLabel
  • Synthesis and biological activity of olomoucine II.
  • Synthesis and biological activity of olomoucine II. (en)
skos:notation
  • RIV/61389030:_____/02:56023048!RIV/2003/GA0/A56003/N
http://linked.open.../vavai/riv/strany
  • 3283;3286
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GA301/02/0475), P(OC 844.10), Z(AV0Z5020903), Z(AV0Z5038910)
http://linked.open...iv/cisloPeriodika
  • 22
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
  • 666105
http://linked.open...ai/riv/idVysledku
  • RIV/61389030:_____/02:56023048
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • purine; olomoucine II; purvalanol A (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [2165FC288625]
http://linked.open...i/riv/nazevZdroje
  • Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...ocetUcastnikuAkce
http://linked.open...nichUcastnikuAkce
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 12
http://linked.open...iv/tvurceVysledku
  • Havlíček, Libor
  • Kuzma, Marek
  • Kryštof, Vladimír
  • Strnad, Miroslav
  • Lenobel, R.
http://linked.open...n/vavai/riv/zamer
issn
  • 0960-894X
number of pages
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