Mostrar el registro sencillo del ítem

Synthesis and evaluation of the cytotoxic activity of novel ethyl 4-[4-(4-substitutedpiperidin-1-yl)]benzyl-phenylpyrrolo[1,2-a]quinoxaline-carboxylate derivatives in myeloid and lymphoid leukemia cell lines

hal.structure.identifierCellules souches hématopoïétiques normales et leucémiques
dc.contributor.authorDESPLAT, Vanessa
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
hal.structure.identifierDepartment of Pharmacy and CIRPeB
dc.contributor.authorVINCENZI, Marian
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorLUCAS, Romain
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorMOREAU, Stéphane
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorSAVRIMOUTOU, Solène
hal.structure.identifierInstitut des Sciences Moléculaires [ISM]
dc.contributor.authorPINAUD, Noël
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorLESBORDES, Jordi
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorPEYRILLES, 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.identifierDepartment of Pharmacy and CIRPeB
dc.contributor.authorROSSI, Filomena
hal.structure.identifierLaboratoire de Glycochimie, des Antimicrobiens et des Agro-ressources - UMR CNRS 7378 [LG2A ]
dc.contributor.authorSONNET, Pascal
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorRONGA, Luisa
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorGUILLON, Jean
dc.date.issued2016
dc.identifier.issn0223-5234
dc.description.abstractEnLeukemia is the most common blood cancer, and its development starts at diverse points, leading to distinct subtypes that respond differently to therapy. This heterogeneity is rarely taken into account in therapies, so it is still essential to look for new specific drugs for leukemia subtypes or even for therapy-resistant cases. Among heterocyclic compounds that attracted a lot of attention because of its wide spread biological activities, the pyrrolo[1,2-a]quinoxaline heterocyclic framework has been identified as interesting scaffolds for antiproliferative activity against various human cancer cell lines. In the present study, novel ethyl 4-[4-(4-substitutedpiperidin-1-yl)]benzyl-phenylpyrrolo[1,2-a]quinoxaline-carboxylate derivatives 1a-l have been designed and synthesized. Their cytotoxicities were evaluated against five different leukemia cell lines, including Jurkat and U266 (lymphoid cell lines), and K562, U937, HL60 (myeloid cell lines), as well as normal human peripheral blood mononuclear cells (PBMNCs). Then, apoptosis study was performed with the more interesting compounds. The new pyrrolo[1,2-a]quinoxaline series showed promising cytotoxic potential against all leukemia cell lines tested, and some compounds showed better results than the reference compound A6730. Some compounds, such as 1a, 1e, 1g and 1h are promising because of their high activity against leukemia and their low activity against normal hematopoietic cells. Structure-activity relationships of these new synthetic compounds 1a-l are here also discussed.
dc.language.isoen
dc.publisherElsevier
dc.subject.enCancer
dc.subject.enCytotoxic activity
dc.subject.enLeukemia
dc.subject.enPyrrolo[1
dc.subject.en2-a]quinoxaline
dc.subject.enSynthesis
dc.title.enSynthesis and evaluation of the cytotoxic activity of novel ethyl 4-[4-(4-substitutedpiperidin-1-yl)]benzyl-phenylpyrrolo[1,2-a]quinoxaline-carboxylate derivatives in myeloid and lymphoid leukemia cell lines
dc.typeArticle de revue
dc.identifier.doi10.1016/j.ejmech.2016.02.047
dc.subject.halChimie/Matériaux
bordeaux.journalEuropean Journal of Medicinal Chemistry
bordeaux.page214-227
bordeaux.volume113
bordeaux.peerReviewedoui
hal.identifierhal-01307573
hal.version1
hal.popularnon
hal.audienceInternationale
hal.origin.linkhttps://hal.archives-ouvertes.fr//hal-01307573v1
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=European%20Journal%20of%20Medicinal%20Chemistry&rft.date=2016&rft.volume=113&rft.spage=214-227&rft.epage=214-227&rft.eissn=0223-5234&rft.issn=0223-5234&rft.au=DESPLAT,%20Vanessa&VINCENZI,%20Marian&LUCAS,%20Romain&MOREAU,%20St%C3%A9phane&SAVRIMOUTOU,%20Sol%C3%A8ne&rft.genre=article


Archivos en el ítem

ArchivosTamañoFormatoVer

No hay archivos asociados a este ítem.

Este ítem aparece en la(s) siguiente(s) colección(ones)

Mostrar el registro sencillo del ítem