Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4365-9. doi: 10.1016/j.bmcl.2003.08.080.

Abstract

A series of (4-chlorophenyl)-alpha-(1-methyl-1H-imidazol-5-yl)azoloquinolines and -quinazolines was prepared. These compounds displayed potent Farnesyl Protein Transferase inhibitory activity and tetrazolo[1,5-a]quinazolines are promising agents for oral in vivo inhibition.

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Animals
  • Cell Division / drug effects
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology*
  • Farnesyltranstransferase
  • Kinetics
  • Molecular Conformation
  • Molecular Structure
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology*
  • Quinolines / chemical synthesis*
  • Quinolines / pharmacology*
  • Quinolones / chemical synthesis
  • Quinolones / pharmacology
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Quinazolines
  • Quinolines
  • Quinolones
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase
  • tipifarnib