Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis

Bioorg Med Chem Lett. 2002 Sep 16;12(18):2545-8. doi: 10.1016/s0960-894x(02)00516-4.

Abstract

A series of novel phenolic compounds has been discovered as potent inhibitors of TNF-alpha-inducible expression of vascular cell adhesion molecule-1 (VCAM-1) with concurrent antioxidant and lipid-modulating properties. Optimization of these multifunctional agents led to the identification of 3a (AGI-1067) as a clinical candidate with demonstrated efficacies in animal models of atherosclerosis and hyperlipidemia.

MeSH terms

  • Animals
  • Antioxidants / pharmacology*
  • Antioxidants / therapeutic use
  • Arteriosclerosis / drug therapy
  • Arteriosclerosis / metabolism*
  • Humans
  • Phenols / pharmacology*
  • Phenols / therapeutic use
  • Tumor Necrosis Factor-alpha / antagonists & inhibitors
  • Vascular Cell Adhesion Molecule-1 / metabolism*

Substances

  • Antioxidants
  • Phenols
  • Tumor Necrosis Factor-alpha
  • Vascular Cell Adhesion Molecule-1