2. Academic Validation
  3. 2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors

2,6,8,9-tetrasubstituted purines as new CDK1 inhibitors

  • Bioorg Med Chem Lett. 2003 Sep 15;13(18):2993-6. doi: 10.1016/s0960-894x(03)00632-2.
Jirí Moravec 1,  Vladimír Krystof,  Jan Hanus,  Libor Havlícek,  Daniela Moravcová,  Kvetoslava Fuksová,  Marek Kuzma,  René Lenobel,  Michal Otyepka,  Miroslav Strnad
Affiliations

Affiliation

  • 1 Isotope Laboratory, Institute of Experimental Botany, Academy of Sciences of the Czech Republic, Vídenská 1083, 14220 Prague 4, Czech Republic.
PMID: 12941319 DOI: 10.1016/s0960-894x(03)00632-2
Abstract

Purine inhibitors of cyclin-dependent kinases attract attention as potential Anticancer drugs because their first representative roscovitine recently entered clinical trials. Although well described in terms of structure-activity relationships, we still present here a novel modification of the purine scaffold influencing their inhibitory properties. The introduced C-8 substituents, however, lowered the CDK inhibitory activity of roscovitine, whereas the antiproliferative potential of several derivatives remained high.

Figures