5-imidazolyl-quinolinones, -quinazolinones and -benzo-azepinones as farnesyltransferase inhibitors

Bioorg Med Chem Lett. 2003 May 5;13(9):1543-7. doi: 10.1016/s0960-894x(03)00180-x.

Abstract

The evaluation of structure-activity relationships associated with the modification of the R115777 quinolinone ring moiety displaying potent in vitro inhibiting activity is described.

MeSH terms

  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Azepines / chemical synthesis*
  • Azepines / chemistry
  • Azepines / pharmacology
  • Farnesyltranstransferase
  • Humans
  • In Vitro Techniques
  • Indicators and Reagents
  • Mice
  • Microsomes, Liver / drug effects
  • Microsomes, Liver / metabolism
  • Quinazolines / chemical synthesis
  • Quinazolines / chemistry*
  • Quinazolines / pharmacology
  • Quinolones / chemical synthesis
  • Quinolones / chemistry*
  • Quinolones / pharmacology
  • Structure-Activity Relationship
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Azepines
  • Indicators and Reagents
  • Quinazolines
  • Quinolones
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase
  • tipifarnib