Montagner, Diego and Gandin, Valentina and Marzano, Cristina and Erxleben, Andrea
(2014)
Phosphate Diester Cleavage, DNA Interaction and
Cytotoxic Activity of a Bimetallic Bis(1,4,7-triazacyclononane)
Zinc Complex.
European Journal of Inorganic Chemistry, 2014 (25).
pp. 4084-4092.
ISSN 1434-1948
Abstract
The dinuclear zinc complex [Zn2{bcmp(-H)}(μ-Cl)](ClO4)2·
H2O {bcmp = 2,6-bis(1,4,7-triazacyclonon-1-ylmethyl)-4-
methylphenol} has been synthesized and structurally characterized.
The DNA binding affinity was assessed by ethidium
bromide fluorescence quenching experiments. The complex
relaxes supercoiled pUC19 DNA into the nicked form at low
micromolar concentration. Mechanistic studies were carried
out using the DNA and RNA models bis(2,4-dinitrophenyl)
phosphate (BDNPP) and 2-hydroxypropyl p-nitrophenyl phosphate (HPNP). A detailed kinetic analysis suggested
that the bridging OH group of the solution species
[Zn2{bcmp(-H)}(μ-OH)]2+ acts as the nucleophile in the hydrolysis
of BDNPP, while in the case of HPNP, the bridging
OH group acts as a general base and seems to shift to a terminal
position upon substrate coordination. Finally, the cytotoxicity
profile of the dinuclear zinc(II) complex was assessed.
The complex showed promising in vitro antitumour
activity against pancreatic and lung cancers cell lines.
| Item Type: |
Article
|
| Keywords: |
Drug design; Antitumor agents; Cytotoxicity; Zinc; DNA; DNA cleavage; |
| Academic Unit: |
Faculty of Science and Engineering > Chemistry |
| Item ID: |
7816 |
| Identification Number: |
https://doi.org/10.1002/ejic.201402319 |
| Depositing User: |
Diego Montagner
|
| Date Deposited: |
26 Jan 2017 16:47 |
| Journal or Publication Title: |
European Journal of Inorganic Chemistry |
| Publisher: |
Wiley |
| Refereed: |
Yes |
| Funders: |
European Commission, Science Foundation Ireland (SFI) |
| URI: |
|
| Use Licence: |
This item is available under a Creative Commons Attribution Non Commercial Share Alike Licence (CC BY-NC-SA). Details of this licence are available
here |
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