Synthesis and biological evaluation of 4-[3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile as novel farnesyltransferase inhibitor

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1293-6. doi: 10.1016/s0960-894x(03)00122-7.

Abstract

Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogues of the potent FTI, 4-[3-biphenyl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile, were synthesized and tested in vitro for their inhibitory activities. The synthesis and detailed biological data of this series of analogues are presented.

MeSH terms

  • 3T3 Cells
  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Farnesyltranstransferase
  • Genes, ras / drug effects
  • Humans
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology*
  • Mice
  • Nitriles / chemical synthesis*
  • Nitriles / pharmacology*
  • Structure-Activity Relationship
  • gamma-Glutamyltransferase / antagonists & inhibitors

Substances

  • 4-(3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl)-1-yl-benzonitrile
  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Imidazoles
  • Nitriles
  • gamma-Glutamyltransferase
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase