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Master Thesis

Conception, synthèse et évaluation biologique d’inhibiteurs potentiels de la voie de signalisation de la sérine / thréonine kinase akt à visée anticancéreuse

Abstract : Attenuation of protein kinases by selective inhibitors is an extremely active field of activity in anticancer drug development. Therefore, Akt, a serine/threonine protein kinase, also known as protein kinase B (PKB), represents an attractive potential target for therapeutic intervention. Recent efforts in the development and biological evaluation of small molecule inhibitors of Akt have led to the identification of novel inhibitors with various heterocycle scaffolds. Based on previous results obtained on the antiproliferative activities of new pyrrolo[1,2-a]quinoxalines, a novel series was designed and synthesized from various substituted phenyl-1H-pyrrole-2-carboxylic acid alkyl esters via multistep heterocyclization process.These new compounds were tested for their in vitro ability to inhibit the proliferation of the human leukemic cell lines HL60, Jurkat, K562, U266 and U937. The first biological evaluation of our new substituted pyrrolo[1,2-a]quinoxalines showed antiproliferative activity against the tested cell lines. These preliminary biological results enlightened the importance of the substitution of the pyrroloquinoxaline scaffold and the functionalisation on the pyrrole ring.
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Master Thesis
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https://dumas.ccsd.cnrs.fr/dumas-01235521
Contributor : Bu Carreire Université de Bordeaux <>
Submitted on : Monday, November 30, 2015 - 11:39:22 AM
Last modification on : Wednesday, August 23, 2017 - 4:32:58 PM
Long-term archiving on: : Tuesday, March 1, 2016 - 12:21:48 PM

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Romain Lucas. Conception, synthèse et évaluation biologique d’inhibiteurs potentiels de la voie de signalisation de la sérine / thréonine kinase akt à visée anticancéreuse. Sciences pharmaceutiques. 2015. ⟨dumas-01235521⟩

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