Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5057-62. doi: 10.1016/j.bmcl.2004.07.083.

Abstract

Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogs of the potent FTI, 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 29 that possesses potent enzymatic and cellular activities.

Publication types

  • Comparative Study

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / pharmacology
  • Biological Availability
  • Biphenyl Compounds / chemical synthesis*
  • Biphenyl Compounds / chemistry
  • Biphenyl Compounds / pharmacokinetics
  • Biphenyl Compounds / pharmacology
  • Farnesyltranstransferase
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Imidazoles / pharmacokinetics
  • Imidazoles / pharmacology
  • In Vitro Techniques
  • Rats
  • Structure-Activity Relationship

Substances

  • 1-benzyl-5-(3-biphenyl-2-ylpropyl)-1H-imidazole
  • Antineoplastic Agents
  • Biphenyl Compounds
  • Imidazoles
  • Alkyl and Aryl Transferases
  • geranylgeranyltransferase type-I
  • Farnesyltranstransferase