DNA binding studies and cytotoxicity of a dinuclear PtII diazapyrenium-based metallo-supramolecular rectangular box

Alessio Terenzi, Cosimo Ducani, Víctor Blanco, Lenka Zerzankova, Aron F. Westendorf, Carlos Peinador, José M. Quintela, Patrick J. Bednarski, Giampaolo Barone, Michael J. Hannon

Research output: Contribution to journalArticlepeer-review

29 Citations (Scopus)

Abstract

The interaction with native DNA of a 2,7-diazapyrenium-based ligand 1 and its PtII rectangular metallacycle 2 is explored through circular and linear dichroism and fluorescence spectroscopies. The metal-free ligand 1 binds through intercalation, with a binding constant of approximately 5 × 105a M-1, whereas the metallacycle 2 binds and bends the DNA with a binding constant of 7 × 106a M-1. PCR assays show that metallo-supramolecular box 2 interferes with DNA transactions in vitro whereas the intercalator 1 does not. The metallacycle is active against four human cancer cell lines, with IC50 values ranging between 3.1 and 19.μ M and shows similar levels of efficacy, but a different spectrum of activity, to cisplatin. Boxed in: Supramolecular boxes bind DNA, prevent DNA transactions and inhibit growth of cancer cells. The interaction of a 2,7-diazapyrenium-based ligand and its PtII rectangular metallacycle with native DNA (see scheme) was explored. The metallacycle is active against four human cancer cell lines, and shows similar levels of efficacy, but a different spectrum of activity, to cisplatin.

Original languageEnglish
Pages (from-to)10983-10990
Number of pages8
JournalChemistry - A European Journal
Volume18
Issue number35
DOIs
Publication statusPublished - 27 Aug 2012

Keywords

  • cytotoxicity
  • metallodrugs
  • noncovalent DNA binding
  • Pt rectangular box
  • supramolecular chemistry

ASJC Scopus subject areas

  • Chemistry(all)

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