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Synthesis and antiproliferative effect of ethyl 4-[4-(4-substituted piperidin-1-yl)]benzylpyrrolo[1,2-a]quinoxalinecarboxylate derivatives on human leukemia cells

hal.structure.identifierCellules souches hématopoïétiques normales et leucémiques
hal.structure.identifierUFR des Sciences Pharmaceutiques
dc.contributor.authorDESPLAT, Vanessa
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierDepartment of Pharmacy and CIRPeB
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorVINCENZI, Marian
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorLUCAS, Romain
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorMOREAU, Stéphane
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorSAVRIMOUTOU, Solène
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorRUBIO, Sandra
hal.structure.identifierInstitut des Sciences Moléculaires [ISM]
dc.contributor.authorPINAUD, Noël
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorBIGAT, David
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorENRIQUEZ, Elodie
hal.structure.identifierInstitut de Chimie de la Matière Condensée de Bordeaux [ICMCB]
dc.contributor.authorMARCHIVIE, Mathieu
hal.structure.identifierInstitut de Chimie Organique et Analytique [ICOA]
dc.contributor.authorROUTIER, Sylvain
hal.structure.identifierLaboratoire de Glycochimie, des Antimicrobiens et des Agro-ressources - UMR CNRS 7378 [LG2A ]
dc.contributor.authorSONNET, Pascal
hal.structure.identifierDepartment of Pharmacy and CIRPeB
dc.contributor.authorROSSI, Filomena
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorRONGA, Luisa
hal.structure.identifierUFR des Sciences Pharmaceutiques
hal.structure.identifierAcides Nucléiques : Régulations Naturelle et Artificielle [ARNA]
dc.contributor.authorGUILLON, Jean
dc.date.issued2017-06-21
dc.identifier.issn1860-7179
dc.description.abstractEnAcute leukemia is a hematological malignancy with high incidence and recurrence rates and is characterized by an accumulation of blasts in bone marrow due to proliferation of immature lymphoid or myeloid cells associated with a blockade of differentiation. The heterogeneity of leukemia led us to look for new specific molecules for leukemia subtypes or for therapy-resistant cases. Among heterocyclic derivatives that attracted attention due to their wide range of biological activities, we focused our interest on the pyrrolo[1,2-a]quinoxaline heterocyclic framework that has been previously identified as an interesting scaffold for antiproliferative activities against various human cancer cell lines. In this work, new ethyl 4-[4-(4-substituted piperidin-1-yl)]benzylpyrrolo[1,2-a]quinoxalinecarboxylate derivatives (1 a-o) were designed, synthesized, and evaluated against five different leukemia cell lines, including Jurkat and U266 (lymphoid cell lines) and K562, U937, and HL60 (myeloid cell lines), as well as on normal human peripheral blood mononuclear cells (PBMCs). This new pyrrolo[1,2-a]quinoxaline series showed interesting cytotoxic potential against all tested leukemia cell lines. In particular, pyrroloquinoxalines 1 a and 1 m,n seem to be interesting due to their high activity against leukemia and their low activity against normal hematopoietic cells, leading to a high index of selectivity.
dc.language.isoen
dc.publisherWiley-VCH Verlag
dc.subject.enanticancer agents
dc.subject.encytotoxic activity
dc.subject.enleukemia
dc.subject.enpyrrolo[1
dc.subject.en2-a]quinoxalines
dc.subject.ensynthesis
dc.title.enSynthesis and antiproliferative effect of ethyl 4-[4-(4-substituted piperidin-1-yl)]benzylpyrrolo[1,2-a]quinoxalinecarboxylate derivatives on human leukemia cells
dc.typeArticle de revue
dc.identifier.doi10.1002/cmdc.201700049
dc.subject.halChimie/Matériaux
bordeaux.journalChemMedChem
bordeaux.page940-953
bordeaux.volume12
bordeaux.issue12
bordeaux.peerReviewedoui
hal.identifierhal-01560237
hal.version1
hal.popularnon
hal.audienceInternationale
hal.origin.linkhttps://hal.archives-ouvertes.fr//hal-01560237v1
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