Jump to main content
Jump to site search
Access to RSC content Close the message box

Continue to access RSC content when you are not at your institution. Follow our step-by-step guide.


Issue 125, 2015
Previous Article Next Article

Novel metal chelators thiosemicarbazones with activity at the σ2 receptors and P-glycoprotein: an innovative strategy for resistant tumor treatment

Author affiliations

Abstract

To combat the emergence of drug-resistance in tumors novel strategies are urgently needed. With this in mind we designed a novel class of thiosemicarbazones able to target simultaneously σ2 receptors and P-glycoprotein efflux pump while chelating metals such as iron. The combined effect of these targets would lead to the activation of multiple pathways to which resistant tumors are sensitive. Indeed, most of the novel thiosemicarbazones displayed antiproliferative activity in both parent (MCF7 breast adenocarcinoma and A549 lung carcinoma) and corresponding doxorubicin-resistant cells (MCF7dx and A549dx). A few compounds emerged for their potent antiproliferative activity or for their more potent effect in doxorubicin-resistant cells than in the parent ones, while other compounds emerged for their remarkable P-gp modulatory activity. These results pave the way for further studies on these targets in the oncology field, while the availability of promising molecules for resistant tumors treatment that warrant deeper investigations was increased.

Graphical abstract: Novel metal chelators thiosemicarbazones with activity at the σ2 receptors and P-glycoprotein: an innovative strategy for resistant tumor treatment

Back to tab navigation

Associated articles

Supplementary files

Article information


Submitted
25 Sep 2015
Accepted
25 Nov 2015
First published
26 Nov 2015

RSC Adv., 2015,5, 103131-103146
Article type
Paper

Novel metal chelators thiosemicarbazones with activity at the σ2 receptors and P-glycoprotein: an innovative strategy for resistant tumor treatment

M. L. Pati, M. Niso, S. Ferorelli, C. Abate and F. Berardi, RSC Adv., 2015, 5, 103131
DOI: 10.1039/C5RA19857G

Social activity

Search articles by author

Spotlight

Advertisements