Structure-activity relationship studies of flavopiridol analogues

Bioorg Med Chem Lett. 2000 May 15;10(10):1037-41. doi: 10.1016/s0960-894x(00)00156-6.

Abstract

Cyclin dependent kinases (CDKs) along with the complementary cyclins form key regulatory checkpoint controls on the cell cycle. Flavopiridol is a synthetic flavone that shows potent and selective cyclin-dependent kinase inhibitory activity. In this paper, we report modifications of the 3-hydroxy-1-methylpiperidinyl (D ring) of flavopiridol and their effect on CDK inhibitory activity.

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Chromones / chemical synthesis
  • Chromones / chemistry*
  • Chromones / pharmacology*
  • Cyclin-Dependent Kinases / antagonists & inhibitors
  • Drug Screening Assays, Antitumor
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Flavonoids / chemistry*
  • Flavonoids / metabolism
  • Flavonoids / pharmacology*
  • Piperidines / chemistry*
  • Piperidines / metabolism
  • Piperidines / pharmacology*
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Pyridines / pharmacology*
  • Structure-Activity Relationship*
  • Tumor Cells, Cultured

Substances

  • 2-(2-chlorophenyl)-5,7-dihydroxy-8-(2,3,6-trihydro-1-methylpyridin-4-yl)benzopyran-4-one
  • Antineoplastic Agents
  • Chromones
  • Enzyme Inhibitors
  • Flavonoids
  • Piperidines
  • Pyridines
  • alvocidib
  • Cyclin-Dependent Kinases