Title: Exploration of the effect of sterically demanding 3'-amido substitution of 3'-deoxyadenosines towards inhibition of cyclin-dependent kinase 1
Authors: Van Calenbergh, Serge ×
Link, A
Kunick, C
Herdewijn, Piet #
Issue Date: 1999
Series Title: Die Pharmazie vol:54 issue:10 pages:727-729
Abstract: 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.
ISSN: 0031-7144
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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