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Towards the synthesis of bisubstrate inhibitors of protein farnesyltransferase: Synthesis and biological evaluation of new farnesylpyrophosphate analogues.

Abstract
Protein farnesyltransferase (FTase) has recently appeared as a new target of parasitic diseases, a field poor in drugs in development. With the aim of creating new bisubstrate inhibitors of FTase, new farnesyl pyrophosphate analogues have been studied. Farnesyl analogues with a malonic acid function exhibited the best inhibitory activity on FTase. This group was introduced into our imidazole-containing model leading to new compounds with submicromolar activities. Kinetic experiments have been realized to determine their binding mode to the enzyme.
AuthorsStéphanie Duez, Laëtitia Coudray, Elisabeth Mouray, Philippe Grellier, Joëlle Dubois
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 18 Issue 2 Pg. 543-56 (Jan 15 2010) ISSN: 1464-3391 [Electronic] England
PMID20036564 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright 2009 Elsevier Ltd. All rights reserved.
Chemical References
  • Polyisoprenyl Phosphates
  • Sesquiterpenes
  • farnesyl pyrophosphate
  • Farnesyltranstransferase
Topics
  • Binding Sites
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Drug Screening Assays, Antitumor
  • Farnesyltranstransferase (antagonists & inhibitors)
  • Humans
  • Kinetics
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum (drug effects, growth & development)
  • Polyisoprenyl Phosphates (chemical synthesis, chemistry, pharmacology)
  • Sesquiterpenes (chemical synthesis, chemistry, pharmacology)
  • Stereoisomerism
  • Structure-Activity Relationship
  • Trypanosoma brucei brucei (drug effects, growth & development)

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