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

Bioorg Med Chem Lett

Isotope Laboratory, Institute of Experimental Botany, Academy of Sciences of the Czech Republic, Vídenská 1083, 14220 Prague 4, Czech Republic.

Published: September 2003

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.

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http://dx.doi.org/10.1016/s0960-894x(03)00632-2DOI Listing

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