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Synthèse de composés hétérocycliques aromatiques azotés, inhibiteurs potentiels de kinases

Abstract : Recently, kinase inhibitors have demonstrated their activities in antitumor therapy and some of them are currently on the market. Thus, we are interested in the preparation of ATP competitive kinase inhibitors with indoline-2-one moities. In the first part, three major kinase families and their involvement in various cellular processes are described. Then, the main families of inhibitors with indolin-2-one moities are detailed. Finally, a description of the different families of inhibitors previously prepared in the laboratory as well as their biological activity is presented. Taking into account the biological results previously obtained, a structure-activity relationship study was pursued on four different families of compounds : acetylated glycosylisoindigos, acetylated glycosyl-7'-azaisoindigos, indolin-2-one substituted in the 3-position by a side-chain containing an 1-amino acid group and tetracyclic pyrrolo-1-carboline. The synthesis of these compounds is presented in the second part. Finally, the antiproliferative activities of the compounds prepared in this work have been determined on different cancer cell lines as well as their inhibitory activity on various kinases. These results are presented in the last part.
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Contributor : Camille Meyer Connect in order to contact the contributor
Submitted on : Wednesday, September 12, 2012 - 4:16:18 PM
Last modification on : Tuesday, December 14, 2021 - 10:38:06 AM
Long-term archiving on: : Thursday, December 13, 2012 - 3:46:59 AM


  • HAL Id : tel-00731331, version 1


Fadoua Bouchikhi. Synthèse de composés hétérocycliques aromatiques azotés, inhibiteurs potentiels de kinases. Chimie de coordination. Université Blaise Pascal - Clermont-Ferrand II, 2008. Français. ⟨NNT : 2008CLF21895⟩. ⟨tel-00731331⟩



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