Pharmazie 1999 Oct 01;5410:727-9.

Exploration of the effect of sterically demanding 3''-amido substitution of 3''-deoxyadenosines towards inhibition of cyclin-dependent kinase 1.

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With focus on exploring the structural demands of adenosine triphosphate pockets of different target enzymes, the 3''-amido-3''-deoxyadenosines 1-7 were synthesized. The inhibitory activity of these compounds on a selected cyclin-dependent kinase as model target in anticancer research was evaluated in vitro. A starfish oocyte enzyme based assay revealed a decreased inhibitory activity in comparison to adenosine. Consequently, the introduction of spacefilling lipophilic 3''-amido substituents alters the enzyme inhibition in an unfavorable manner.

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Genes referenced: cdk1