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Synthèse de nouveaux carbazoles inhibiteurs de la Chk1. Etude de leurs propriétés biologiques

Abstract : The granulatimide and isogranulatimide, natural molecules isolated from a tunicate Didemmum granulatum are known to be inhibitors of Chk1, regulatory enzyme of the checkpoint in G2 cell cycle. The first part of this work is devoted to the presentation of the checkpoint in G2 cell cycle and more particularly to a checkpoint kinase Chk1. In the second part, the synthesis of new analogues of carbazoles granulatimide isogranulatimide and will be described. Among these analogs imide the heterocycle will first be replaced by a lactam, a pyrazolinone, a pyridazine and the heterocycle is imidazole to him when replaced by carbocyclic 5 or 6 membered functionalized. A third section presents the test results of Chk1 inhibition and antiproliferative activity on three cancer cell lines performed on the synthesized analogs. All bioassays were conducted in laboratories Servier.
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https://theses.hal.science/tel-00717338
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Submitted on : Thursday, July 12, 2012 - 3:30:05 PM
Last modification on : Tuesday, December 14, 2021 - 10:38:06 AM
Long-term archiving on: : Saturday, October 13, 2012 - 2:35:31 AM

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  • HAL Id : tel-00717338, version 1

Citation

Elisabeth Conchon. Synthèse de nouveaux carbazoles inhibiteurs de la Chk1. Etude de leurs propriétés biologiques. Chimie organique. Université Blaise Pascal - Clermont-Ferrand II, 2006. Français. ⟨NNT : 2006CLF21711⟩. ⟨tel-00717338⟩

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