Novel CDK inhibition profiles of structurally varied 1-aza-9-oxafluorenes

Bioorg Med Chem Lett. 2005 Feb 1;15(3):823-5. doi: 10.1016/j.bmcl.2004.10.091.

Abstract

A series of 1-aza-9-oxafluorenes with functionally varied 3-substituents have been prepared from N-phenoxycarbonyl-4-phenyl-1,4-dihydropyridines and p-benzoquinone and biologically evaluated as inhibitors of various cyclin-dependant kinases. The absence of a 3-hydrogen bond acceptor function leads to a complete loss of inhibitory activity. Differing hydrogen bond acceptor functions surprisingly cause significant shifts in the selectivity of inhibition profiles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Cyclin-Dependent Kinases / antagonists & inhibitors*
  • Enzyme Inhibitors / chemical synthesis
  • Fluorenes / chemical synthesis*
  • Fluorenes / pharmacology*
  • Humans
  • Hydrogen Bonding
  • Inhibitory Concentration 50
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Fluorenes
  • Cyclin-Dependent Kinases