New indene-derivatives with anti-proliferative properties

Bioorg Med Chem Lett. 2002 Feb 25;12(4):709-13. doi: 10.1016/s0960-894x(01)00839-3.

Abstract

Metabolites of the non-steroidal anti-inflammatory drug Sulindac inhibit cell proliferation by affecting several intracellular signaling pathways including the tumorigenic Ras/Raf/MAPK pathway. Here, we report the synthesis of eight new indene derivatives derived from the Sulindac structure, and present data on their anti-proliferative properties and their effects on the p21ras protein.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Cell Division / drug effects
  • Combinatorial Chemistry Techniques
  • Cyclooxygenase Inhibitors / chemical synthesis
  • Cyclooxygenase Inhibitors / pharmacology
  • Dogs
  • Humans
  • Indenes / chemical synthesis
  • Indenes / pharmacology*
  • Inhibitory Concentration 50
  • Mice
  • Oncogene Protein p21(ras) / antagonists & inhibitors
  • Oncogene Protein p21(ras) / drug effects
  • Prostaglandin-Endoperoxide Synthases / drug effects
  • Sulindac / analogs & derivatives*
  • Tumor Cells, Cultured / drug effects

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Antineoplastic Agents
  • Cyclooxygenase Inhibitors
  • Indenes
  • Sulindac
  • Prostaglandin-Endoperoxide Synthases
  • Oncogene Protein p21(ras)