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RESEARCH PRODUCT
Structural basis for the potential antitumour activity of DNA-interacting benzo[kl]xanthene lignans
Norbert LatruffeSimone Di MiccoDominique DelmasFrédéric MazuéGiuseppe BifulcoCarmela SpataforaCorrado TringaliRaffaele RiccioCarmelo Daquinosubject
XantheneModels MolecularStereochemistryCell SurvivalMetaboliteAntinematodal AgentsOrganic ChemistryDNABiochemistryIn vitroLignanschemistry.chemical_compoundInhibitory Concentration 50Structure-Activity RelationshipchemistryXanthenesBiological propertyCell Line TumorHumansNucleic Acid ConformationPhysical and Theoretical ChemistryCancer cell linesDNAdescription
The biological properties and possible pharmacological applications of benzo[kl]xanthene lignans, rare among natural products and synthetic compounds, are almost unexplored. In the present contribution, the possible interaction of six synthetic benzo[kl]xanthene lignans and the natural metabolite rufescidride with DNA has been investigated through a combined STD-NMR and molecular docking approach, paralleled by in vitro biological assays on their antiproliferative activity towards two different cancer cell lines: SW 480 and HepG2. Our data suggest that the benzo[kl]xanthene lignans are suitable lead compounds for the design of DNA selective ligands with potential antitumour properties.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2010-11-17 |