Jump to main content
Jump to site search

Issue 12, 2015
Previous Article Next Article

Discovery of a dual-targeting organometallic ruthenium complex with high activity inducing early stage apoptosis of cancer cells

Author affiliations

Abstract

Ruthenium based complexes are promising antitumour candidates due to their lower toxicity and better water-solubility compared to the platinum antitumour complexes. An epidermal growth factor receptor (EGFR) has been found to be overexpressed in a large set of tumour cells. In this work, a series of organoruthenium complexes containing EGFR-inhibiting 4-anilinoquinazoline pharmacophores were synthesised and characterised. These complexes exhibited excellent inhibitory activity against EGFR and high affinity to interact with DNA via minor groove binding, featuring dual-targeting properties. In vitro screening demonstrated that the as-prepared ruthenium complexes are anti-proliferating towards a series of cancer cell lines, in particular the non-small-cell lung cancer cell line A549. Fluorescence-activated cell sorting analysis and fluorescence microscopy revealed that the most active complex 3 induced much more early-stage cell apoptosis than its cytotoxic arene ruthenium analogue and the EGFR-inhibiting 4-anilinoquinazolines, verifying the synergetic effect of the two mono-functional pharmacophores.

Graphical abstract: Discovery of a dual-targeting organometallic ruthenium complex with high activity inducing early stage apoptosis of cancer cells

Back to tab navigation

Supplementary files

Publication details

The article was received on 14 May 2015, accepted on 28 Sep 2015 and first published on 28 Sep 2015


Article type: Paper
DOI: 10.1039/C5MT00122F
Author version
available:
Download author version (PDF)
Metallomics, 2015,7, 1573-1583

  •   Request permissions

    Discovery of a dual-targeting organometallic ruthenium complex with high activity inducing early stage apoptosis of cancer cells

    J. Du, E. Zhang, Y. Zhao, W. Zheng, Y. Zhang, Y. Lin, Z. Wang, Q. Luo, K. Wu and F. Wang, Metallomics, 2015, 7, 1573
    DOI: 10.1039/C5MT00122F

Search articles by author

Spotlight

Advertisements