Issue 3, 2011
From the journal:

Organic & Biomolecular Chemistry

Structural basis for the potential antitumour activity of DNA-interacting benzo[kl]xanthenelignans†

Simone Di Micco,a   Frédéric Mazué,b   Carmelo Daquino,c   Carmela Spatafora,c   Dominique Delmas,b   Norbert Latruffe,b   Corrado Tringali,c   Raffaele Riccioa  and  Giuseppe Bifulco*a  

* Corresponding authors

a Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, Fisciano (SA), Italy
E-mail: bifulco@unisa.it
Fax: +39 089 969602
Tel: +39 089 969741

b INSERM U 866, University of Burgundy, Laboratory of Biochemistry of Metabolism and Nutrition, 6, Bd Gabriel, Dijon, France

c Dipartimento di Scienze Chimiche, Università degli Studi di Catania, Viale A. Doria 6, Catania, Italy

Abstract

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.

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

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Article information

DOI
https://doi.org/10.1039/C0OB00480D
Article type
Paper
Submitted
23 Jul 2010
Accepted
29 Sep 2010
First published
04 Oct 2010

Org. Biomol. Chem., 2011,9, 701-710

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

S. Di Micco, F. Mazué, C. Daquino, C. Spatafora, D. Delmas, N. Latruffe, C. Tringali, R. Riccio and G. Bifulco, Org. Biomol. Chem., 2011, 9, 701 DOI: 10.1039/C0OB00480D

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