Diaryl ether inhibitors of farnesyl-protein transferase

Bioorg Med Chem Lett. 2001 May 21;11(10):1257-60. doi: 10.1016/s0960-894x(01)00162-7.

Abstract

Imidazolemethyl diaryl ethers are potent inhibitors of farnesyl-protein transferase. The SNAr displacement reaction used to prepare these diaryl ethers was amenable to rapid parallel synthesis of FPTase inhibitors. The use of a broad range of commercially available phenols quickly identified compounds which proved active in cells.

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Alkyl and Aryl Transferases / metabolism
  • Animals
  • Binding, Competitive
  • Cell Line
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Imidazoles / chemistry
  • Inhibitory Concentration 50
  • Peptide Library
  • Phenyl Ethers / chemical synthesis
  • Phenyl Ethers / pharmacology*
  • Rats
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Imidazoles
  • Peptide Library
  • Phenyl Ethers
  • Alkyl and Aryl Transferases
  • geranylgeranyltransferase type-I
  • p21(ras) farnesyl-protein transferase