Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors

Bioorg Med Chem Lett. 2012 Feb 15;22(4):1678-81. doi: 10.1016/j.bmcl.2011.12.112. Epub 2011 Dec 30.

Abstract

Compounds belonging to several scaffolds-quinazolines, quinolines and quinoxalines-were designed and synthesized as Raf kinase inhibitors. Scaffolds were assessed for in vitro Braf(V600E) inhibition, and overall kinase selectivity. Pharmacokinetic parameters for one of the scaffolds were also determined.

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Amides / pharmacology*
  • Binding Sites
  • Cells, Cultured
  • Drug Design*
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Heterocyclic Compounds / chemical synthesis
  • Heterocyclic Compounds / chemistry
  • Heterocyclic Compounds / pharmacology
  • Humans
  • Models, Molecular
  • Molecular Structure
  • raf Kinases / antagonists & inhibitors*

Substances

  • Amides
  • Enzyme Inhibitors
  • Heterocyclic Compounds
  • raf Kinases