title: Exploration of the effect of sterically demanding 3'-amido substitution of 3'-deoxyadenosines towards inhibition of cyclin-dependent kinase 1.
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.
authors.affiliation: Faculteit Farmaceutische Wetenschappen, Universiteit Gent, Belgium.
authors.forename: S
authors.initials: S
authors.lastname: Van Calenbergh
authors.forename: A
authors.initials: A
authors.lastname: Link
authors.forename: C
authors.initials: C
authors.lastname: Kunick
authors.forename: P
authors.initials: P
authors.lastname: Herdewijn
mesh_terms: D000818:Animals; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors*; D003839:Deoxyadenosines / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D009865:Oocytes / Q000201:enzymology; D013215:Starfish
chemical_list: D003839:Deoxyadenosines; D004791:Enzyme Inhibitors; D016203:CDC2 Protein Kinase