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Org Biomol Chem. 2011 Feb 7;9(3):701-10. doi: 10.1039/c0ob00480d. Epub 2010 Nov 16.

Structural basis for the potential antitumour activity of DNA-interacting benzo[kl]xanthene lignans.

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Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084, Fisciano (SA), Italy.


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.

[Indexed for MEDLINE]

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