0000000000404292

AUTHOR

Marie-hélène David-cordonnier

showing 2 related works from this author

Photochemical electrocyclisation of 3-vinylindoles to pyrido[2,3-a]-, pyrido[4,3-a]- and thieno[2,3-a]-carbazoles: Design, synthesis, DNA binding and…

2009

In the context of the design and synthesis of DNA ligands, some new hetarene annelated carbazoles were synthesized. As lead structure the intercalating tetracyclic systems pyrido[2,3-a]- and pyrido[4,3-a]-carbazoles and in one case a thieno[2,3-a]-carbazole were taken into account. A dialkyl amino amidic chain was introduced to the planar chromophoric system with the intent to generate minor groove binding properties. The cytotoxicity of some compounds was examined by the NCI antitumor screening. Furthermore, biophysical as well as biochemical studies were performed in order to get some information about the DNA-binding properties and inhibition of DNA related functional enzymes of this new…

IndolesCell SurvivalStereochemistryCarbazolesFluorescence spectrometryAntineoplastic AgentsStereoisomerismContext (language use)Nucleic Acid DenaturationChemical synthesisFluorescenceStructure-Activity RelationshipCell Line TumorDrug DiscoveryAnimalsHumansTopoisomerase II InhibitorsTransition TemperatureStructure–activity relationshipBinding siteCell ProliferationPharmacologyBinding SitesbiologyChemistryCircular DichroismTopoisomeraseCell CycleOrganic ChemistryStereoisomerismDNAGeneral MedicinePhotochemical ProcessesDNA Minor Groove BindingCyclizationDrug Designbiology.proteinCattleSpectrophotometry UltravioletTopoisomerase I InhibitorsEuropean Journal of Medicinal Chemistry
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Design, synthesis and biological evaluation of new oligopyrrole carboxamides linked with tricyclic DNA-intercalators as potential DNA ligands or topo…

2007

In the context of the design and synthesis of minor groove binding and intercalating DNA ligands some new oligopyrrole carboxamides were synthesized. These hybrid molecules (combilexins) possess a variable and conformatively flexible spacer at the N-terminal end. As intercalating tricyclic systems acridone, acridine, anthraquinones and in a special case iminostilbene terminate the N-terminal end of the pyrrole chain. The cytotoxicity was examined by the NCI antitumor screening, furthermore, biophysical as well as biochemical studies were performed in order to get some information about the DNA binding properties and topoisomerase inhibition effect of this new series of molecules.

Stereochemistrymedicine.drug_classTopoisomerase InhibitorsDNA FootprintingContext (language use)Antineoplastic AgentsLigandschemistry.chemical_compoundStructure-Activity RelationshipCell Line TumorDrug DiscoverymedicineStructure–activity relationshipHumansPyrrolesPharmacologybiologyMolecular StructureChemistryTopoisomeraseOrganic ChemistryDistamycinsNetropsinGeneral MedicineDNADNA Minor Groove BindingIntercalating AgentsAcridoneDrug DesignAcridinebiology.proteinTopoisomerase inhibitorDNAEuropean journal of medicinal chemistry
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