4.7 Article

pH and DNA luminescence switching, DNA photocleavage and cytotoxic properties of two thiophene-containing ruthenium(II) complexes

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 87, Issue -, Pages 10-22

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.09.041

Keywords

Ruthenium; DNA; DNA switch; DNA photocleavage; Cytotoxicity

Funding

  1. National Natural Science Foundation of China [21171022]
  2. Program for Innovative Research Team in University, Ministry of Education [IRT13005]
  3. Beijing Normal University

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Two new Ru(II) complexes, [Ru(Htip)(3)]Cl-2 (1) and [Ru(Htip)(2)(dppz)]Cl-2 (2), were synthesised and were characterised. The ground- and excited-state acid-base properties of 1 and 2 were studied and demonstrated that 1 acted as a pH-induced on-off-on luminescence switch. The binding behaviours of 1 and 2 to calf thymus DNA were studied with absorption and emission spectroscopy, DNA viscosities and density functional theory calculations. 2 was found to act as a DNA molecular light switch and as an efficient photocleaver of pUC 18 DNA. The cytotoxicities of the complexes were evaluated with the MTT method and it was found that 1 displayed apparent anticancer activity against MCF-7 cell, whereas 2 exhibited more potent and wider-spectrum antitumor activities against all cancer cell lines tested. (C) 2014 Elsevier Masson SAS. All rights reserved.

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