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Synthèse d'hybrides d'indolocarbazoles et de la caulersine, composés à visée antitumorale

Abstract : Cancer, which is in France the second cause of mortality, is nowadays a major problem of public health and is the subject of manifold researches. Numerous molecules have been synthesized with the aim of finding more efficient and selective drugs with especially less secondary effects. Among these molecules can be found indolocarbazoles, of which rebeccamycin and staurosporine are the most famous representatives. The structure activity relationships (SAR) of this family were studied.
As part of the research of new cytotoxic agents and kinases inhibitors still more selective, the main structure of phenylcarbazoles, compounds from indolocarbazoles' family, was modified by introducing a central tropone, a 7-membered ring with a carbonyl function. The different ways to synthesize this new family of compounds, named oxophenylarcyriaflavines, were explored. The method retained for the final step of the synthesis was electrophilic cyclisation onto carbon C-2 of indole. This synthesis was then generalized for the compounds substituted by hydroxyle groups onto C-5 of indole on one hand and onto C-4' and C-5' of phenyl core on the other hand. 17 final molecules were synthesized and underwent biologically tests which permit to establish SAR for this new family. Finally, this methodology was applied to the synthesis of the first family of bisindolic compounds bearing a central tropone.
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Contributor : Laurent Robin <>
Submitted on : Monday, May 21, 2007 - 12:45:24 PM
Last modification on : Thursday, March 5, 2020 - 6:49:18 PM
Long-term archiving on: : Thursday, April 8, 2010 - 5:13:18 PM


  • HAL Id : tel-00147916, version 1


Aurélie Bourderioux. Synthèse d'hybrides d'indolocarbazoles et de la caulersine, composés à visée antitumorale. Autre. Université d'Orléans, 2007. Français. ⟨tel-00147916⟩



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