Non-thiol farnesyltransferase inhibitors: N-(4-tolylacetylamino-3-benzoylphenyl)-3-arylfurylacrylic acid amides

Bioorg Med Chem. 2004 Sep 1;12(17):4585-600. doi: 10.1016/j.bmc.2004.07.010.

Abstract

We have designed arylfurylacryl-substituted benzophenones as non-thiol farnesyltransferase inhibitors utilizing a novel aryl binding site of farnesyltransferase. These compounds display activity in the low nanomolar range.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylates / chemical synthesis*
  • Acrylates / pharmacology
  • Alkyl and Aryl Transferases / antagonists & inhibitors*
  • Amides / chemical synthesis
  • Amides / pharmacology
  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology
  • Binding Sites
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology
  • Farnesyltranstransferase
  • Inhibitory Concentration 50
  • Rats
  • Saccharomyces cerevisiae / enzymology
  • Structure-Activity Relationship
  • Sulfhydryl Compounds / chemistry

Substances

  • Acrylates
  • Amides
  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Sulfhydryl Compounds
  • Alkyl and Aryl Transferases
  • Farnesyltranstransferase