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Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2.

hal.structure.identifierMolécules bioactives et chimie médicinale [B2MC]
dc.contributor.authorALCHAB, Faten
hal.structure.identifierMolécules bioactives et chimie médicinale [B2MC]
dc.contributor.authorETTOUATI, Laurent
hal.structure.identifierMolécules bioactives et chimie médicinale [B2MC]
dc.contributor.authorBOUAZIZ, Zouhair
hal.structure.identifierInstitut für Pharmazeutische und Medizinische Chemie
dc.contributor.authorBOLLACKE, Andre
hal.structure.identifierCentre de Recherche en Cancérologie de Lyon [UNICANCER/CRCL]
dc.contributor.authorDELCROS, Jean-Guy
hal.structure.identifierPharmakologie und Klinische Pharmakologie
dc.contributor.authorGERTZEN, Christoph G W
hal.structure.identifierPharmakologie und Klinische Pharmakologie
dc.contributor.authorGOHLKE, Holger
hal.structure.identifierInstitut des Sciences Moléculaires [ISM]
dc.contributor.authorPINAUD, Noël
hal.structure.identifierInstitut de Chimie de la Matière Condensée de Bordeaux [ICMCB]
dc.contributor.authorMARCHIVIE, Mathieu
hal.structure.identifierRégulations Naturelles et Artificielles [ARNA]
dc.contributor.authorGUILLON, Jean
hal.structure.identifierUniversité Claude Bernard Lyon 1 [UCBL]
hal.structure.identifierCentre Commun de Résonance Magnétique Nucléaire, Université Lyon1 [CCRMN]
dc.contributor.authorFENET, Bernard
hal.structure.identifierInstitut für Pharmazeutische und Medizinische Chemie
dc.contributor.authorJOSE, Joachim
hal.structure.identifierMolécules bioactives et chimie médicinale [B2MC]
dc.contributor.authorBORGNE, Marc Le
dc.date.issued2015-06-08
dc.identifier.issn1424-8247
dc.description.abstractEnDue to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design of ATP-competitive inhibitors of human CK2. In the present study, we prepared twenty-one indeno[1,2-b]indole derivatives, all of which were tested in vitro on human CK2. The indenoindolones 5a and 5b inhibited human CK2 with an IC50 of 0.17 and 0.61 µM, respectively. The indeno[1,2-b]indoloquinone 7a also showed inhibitory activity on CK2 at a submicromolar range (IC50 = 0.43 µM). Additionally, a large number of indenoindole derivatives was evaluated for their cytotoxic activities against the cell lines 3T3, WI-38, HEK293T and MEF.
dc.language.isoen
dc.publisherMDPI
dc.subject.eninhibitory activity
dc.subject.ensynthesis
dc.subject.enprotein kinase CK2
dc.subject.en2-b]indoles
dc.subject.enindeno[1
dc.subject.encytotoxicity
dc.subject.enmolecular modeling
dc.title.enSynthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2.
dc.typeArticle de revue
dc.identifier.doi10.3390/ph8020279
dc.subject.halChimie/Chemo-informatique
dc.subject.halChimie/Chimie thérapeutique
dc.subject.halSciences du Vivant [q-bio]/Biologie cellulaire
dc.subject.halSciences du Vivant [q-bio]/Cancer
dc.subject.halSciences du Vivant [q-bio]/Sciences pharmaceutiques
dc.subject.halChimie/Cristallographie
dc.subject.halChimie/Matériaux
bordeaux.journalPharmaceuticals
bordeaux.page279-302
bordeaux.volume8
bordeaux.issue2
bordeaux.peerReviewedoui
hal.identifierhal-01164133
hal.version1
hal.popularnon
hal.audienceInternationale
hal.origin.linkhttps://hal.archives-ouvertes.fr//hal-01164133v1
bordeaux.COinSctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Pharmaceuticals&rft.date=2015-06-08&rft.volume=8&rft.issue=2&rft.spage=279-302&rft.epage=279-302&rft.eissn=1424-8247&rft.issn=1424-8247&rft.au=ALCHAB,%20Faten&ETTOUATI,%20Laurent&BOUAZIZ,%20Zouhair&BOLLACKE,%20Andre&DELCROS,%20Jean-Guy&rft.genre=article


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