Thalidomide and its analogues as cyclooxygenase inhibitors

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1043-6. doi: 10.1016/s0960-894x(02)00084-7.

Abstract

Thalidomide showed cyclooxygenase (COX)-1/2 inhibitory activity with a potency comparable to that of aspirin. Structural development studies of thalidomide resulted in potent COX-1/2 inhibitors, and COX-1-selective and COX-2-selective inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / chemistry
  • Cyclooxygenase Inhibitors / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Isoenzymes / antagonists & inhibitors*
  • Isoenzymes / metabolism
  • Membrane Proteins
  • Molecular Structure
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Structure-Activity Relationship
  • Substrate Specificity
  • Thalidomide / analogs & derivatives*
  • Thalidomide / chemical synthesis
  • Thalidomide / pharmacology*

Substances

  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Membrane Proteins
  • Thalidomide
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • PTGS1 protein, human
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases