Structure-activity relationships studies of the anti-angiogenic activities of linomide

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1187-9. doi: 10.1016/s0960-894x(03)00047-7.

Abstract

The synthesis and anti-angiogenic activities of linomide and its analogues are reported. Three of the analogues are 3.3-69 times more potent than linomide at inhibiting blood vessel formation in the CAM angiogenesis assay. These compounds possessed considerable anti-proliferative activity against isolated HUVEC cells with no activity against epithelial-derived prostate tumor cells.

MeSH terms

  • Allantoin / chemistry
  • Angiogenesis Inhibitors / chemical synthesis*
  • Angiogenesis Inhibitors / pharmacology*
  • Animals
  • Cell Division / drug effects
  • Chick Embryo
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects
  • Humans
  • Hydroxyquinolines / chemical synthesis*
  • Hydroxyquinolines / pharmacology*
  • Male
  • Membranes / drug effects
  • Muscle, Smooth, Vascular / cytology
  • Muscle, Smooth, Vascular / drug effects
  • Prostatic Neoplasms / blood supply
  • Prostatic Neoplasms / pathology
  • Regional Blood Flow / drug effects
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • Angiogenesis Inhibitors
  • Hydroxyquinolines
  • Allantoin
  • roquinimex