Jump to main content
Jump to site search

Issue 2, 2016
Previous Article Next Article

Cytotoxicity and preliminary mode of action studies of novel 2-aryl-4-thiopyrone-based organometallics

Author affiliations

Abstract

Organometallic complexes with thiopyrone-based ligands have shown promising cytotoxic activity in vitro. To investigate the impact of the ligand backbone modification of these biologically active compounds and enhance the solubility in aqueous solution, the (thio)pyrone scaffold was modified via Suzuki–Miyaura coupling reaction and converted into corresponding organometallic Ru(II) and Rh(III) complexes. Characterization of the synthesized compounds was carried out by means of 1D and 2D NMR, ESI MS, and also by X-ray diffraction analysis. The stability in aqueous solution was investigated via1H NMR spectroscopy. Due to the close structural resemblance to flavonoids, topoisomerase inhibition, the cytotoxicity in human cancer cell lines as well as ROS generation was investigated by means of the topoisomerase II drug screening assay, the MTT assay and DCFH-DA assay, respectively.

Graphical abstract: Cytotoxicity and preliminary mode of action studies of novel 2-aryl-4-thiopyrone-based organometallics

Back to tab navigation

Supplementary files

Publication details

The article was received on 17 Jul 2015, accepted on 18 Nov 2015 and first published on 02 Dec 2015


Article type: Paper
DOI: 10.1039/C5DT02722E
Citation: Dalton Trans., 2016,45, 724-733
  •   Request permissions

    Cytotoxicity and preliminary mode of action studies of novel 2-aryl-4-thiopyrone-based organometallics

    M. Schmidlehner, L. S. Flocke, A. Roller, M. Hejl, M. A. Jakupec, W. Kandioller and B. K. Keppler, Dalton Trans., 2016, 45, 724
    DOI: 10.1039/C5DT02722E

Search articles by author

Spotlight

Advertisements