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

Pharmazie. 1999 Oct;54(10):727-9.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CDC2 Protein Kinase / antagonists & inhibitors*
  • Deoxyadenosines / chemical synthesis*
  • Deoxyadenosines / pharmacology
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Oocytes / enzymology
  • Starfish

Substances

  • Deoxyadenosines
  • Enzyme Inhibitors
  • CDC2 Protein Kinase