DNA G-rich sequences are able to form four-stranded structures organized in stacked guanine tetrads. These structures, called G-quadruplexes, were found to have an important role in the regulation of oncogenes expression and became, for such a reason, appealing targets for anticancer drugs. Aiming at finding selective G-quadruplex binders, we have designed, synthesized and characterized a new water soluble Salen-like Schiff base ligand and its NiII and CuII metal complexes. UV-Vis, circular dichroism and FRET measurements indicated that the nickel complex can stabilize oncogene promoter G-quadruplexes with high selectivity, presenting no interactions with duplex DNA at all. The same compound exhibited dose-dependent cytotoxic activity in MCF-7 breast cancer cells when combined with lipofectamine as lipophilic carrier.
|Numero di pagine||10|
|Stato di pubblicazione||Published - 2016|
All Science Journal Classification (ASJC) codes
- Inorganic Chemistry
Terenzi, A., Barone, G., Kowol, C. R., Roller, A., Terenzi, A., Lötsch, D., Keppler, B. K., Berger, W., Van Schoonhoven, S., & Barone, G. (2016). Another step toward DNA selective targeting: NiII and CuII complexes of a Schiff base ligand able to bind gene promoter G-quadruplexes. Dalton Transactions, 45, 7758-7767.