Discovery of 2-phenyl-3-sulfonylphenyl-indole derivatives as a new class of selective COX-2 inhibitors

Bioorg Med Chem. 2003 Dec 1;11(24):5539-44. doi: 10.1016/j.bmc.2003.09.008.

Abstract

2-Sulfonylphenyl-3-phenyl-indole derivatives have been reported to be highly potent and selective COX-2 inhibitors previously. In this paper, the regio-isomeric analogues-2-phenyl-3-sulfonylphenyl-indoles were identified as potent and selective COX-2 inhibitors. This work led to the discovery of compounds 4a and 8a possessing higher activity than Celecoxib on cellular assay.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / classification
  • Cyclooxygenase Inhibitors / pharmacology*
  • Indoles / chemical synthesis*
  • Indoles / classification
  • Indoles / pharmacology*
  • Isoenzymes / antagonists & inhibitors*
  • Macrophages, Peritoneal / enzymology
  • Male
  • Membrane Proteins
  • Mice
  • Mice, Inbred C57BL
  • Molecular Structure
  • Prostaglandin-Endoperoxide Synthases

Substances

  • 2-phenyl-3-sulfonylphenyl-indole
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Indoles
  • Isoenzymes
  • Membrane Proteins
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Prostaglandin-Endoperoxide Synthases
  • Ptgs1 protein, mouse