OPTIMISATION EN SYNTHESE PARALLELE SUR PHASE SOLIDE DE QUINAZOLINEDIONES INHIBITRICES DE S-FARNESYLTRANSFERASE

  • KUCHARCZYK NATHALIE
    INSTITUT DE RECHERCHES SERVIER, 125 CHEMIN DE RONDE, 78290 CROISSY-SUR- SEINE, FRANCE
  • TIZOT ANDRÉ
    INSTITUT DE RECHERCHES SERVIER, 11 RUE DES MOULINEAUX, 92150 SURESNES, FRANCE
  • MERER GOULVEN
    INSTITUT DE RECHERCHES SERVIER, 125 CHEMIN DE RONDE, 78290 CROISSY-SUR- SEINE, FRANCE
  • DHAINAUT ALAIN
    INSTITUT DE RECHERCHES SERVIER, 125 CHEMIN DE RONDE, 78290 CROISSY-SUR- SEINE, FRANCE
  • TUCKER C. GORDON
    INSTITUT DE RECHERCHES SERVIER, 125 CHEMIN DE RONDE, 78290 CROISSY-SUR- SEINE, FRANCE
  • FAUCHÈRE JEAN-LUC
    INSTITUT DE RECHERCHES SERVIER, 11 RUE DES MOULINEAUX, 92150 SURESNES, FRANCE
  • GOLDSTEIN SOLO
    INSTITUT DE RECHERCHES SERVIER, 11 RUE DES MOULINEAUX, 92150 SURESNES, FRANCE

Abstract

The discovery of anti-cancer drugs based on the post traductional modification of Ras protein has been thoroughly studied in the last years. The aim of the present study is to optimize the solid phase synthesis of quinazolinediones, compounds that present an inhibitory activity of the S-farnesyltransferaze (FTase). Two strategies for obtaining a new FTase inhibitor, S35028, are presented.

Cuvinte cheie

quinazolinediones FTase inhibitor solid phase synthesis anti-cancer drugs