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Description
| - Cyclin-dependent kinases (CDKs) have raised considerable attention because of their pivotal role in the regulation of cell division cycle. Due to their hyperactivation in a number of transformed cells, drug discovery programs direct the effort towards the identification of chemical inhibitors of CDKs as anticancer agents. In our effort to enhance the affinity of purine inhibitors to CDKs, we introduced another side chain at C8. The straightforward syntheses of 2,6,8,9-tetrasubstituted purines [1-3] generally started from previously synthesised 2,6,9-trisubstituted purines [4,5] and are described in details (see Scheme 1). The inhibitor-CDK mutual interactions between CDK2 and inhibitor were subsequently verified by molecular modelling [6]. The introduced C8 substituents, however, lowered the CDK inhibitory activity, whereas the antiproliferative activity of several derivatives remained high (Tab. 1.).
- Cyclin-dependent kinases (CDKs) have raised considerable attention because of their pivotal role in the regulation of cell division cycle. Due to their hyperactivation in a number of transformed cells, drug discovery programs direct the effort towards the identification of chemical inhibitors of CDKs as anticancer agents. In our effort to enhance the affinity of purine inhibitors to CDKs, we introduced another side chain at C8. The straightforward syntheses of 2,6,8,9-tetrasubstituted purines [1-3] generally started from previously synthesised 2,6,9-trisubstituted purines [4,5] and are described in details (see Scheme 1). The inhibitor-CDK mutual interactions between CDK2 and inhibitor were subsequently verified by molecular modelling [6]. The introduced C8 substituents, however, lowered the CDK inhibitory activity, whereas the antiproliferative activity of several derivatives remained high (Tab. 1.). (en)
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Title
| - Tetrasubstituted purines as inhibitors of CDK1
- Tetrasubstituted purines as inhibitors of CDK1 (en)
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skos:prefLabel
| - Tetrasubstituted purines as inhibitors of CDK1
- Tetrasubstituted purines as inhibitors of CDK1 (en)
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skos:notation
| - RIV/61989592:15310/03:00001584!RIV/2004/GA0/153104/N
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http://linked.open.../vavai/riv/strany
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/61989592:15310/03:00001584
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - purine, inhibitor, CDK1 (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Cellular & Molecular Biology Letters
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...ocetUcastnikuAkce
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http://linked.open...nichUcastnikuAkce
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Hanuš, Jan
- Kryštof, Vladimír
- Otyepka, Michal
- Strnad, Miroslav
- Moravec, J.
- Fuksová, K.
- Havlíček, L.
- Moravcová, D.
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number of pages
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http://localhost/t...ganizacniJednotka
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