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Au(iii)-Proline derivatives exhibiting selective antiproliferative activity against HepG2/SB3 apoptosis-resistant cancer cells

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Abstract

This paper deals with the combination of a proline-based moiety with biologically active gold centers in the oxidation states +1 and +3. In particular, six Au(I)/(III)–proline dithiocarbamato (DTC) complexes with general formulae [AuI2(DTC)2] and [AuIIIX2(DTC)] (X = Cl, Br) are reported here. After the synthesis of the ligand and the complexes, all derivatives were characterized via several techniques and tested for their stability in DMSO/water media. This study was focused on the demonstration of a peculiar behavior of Au(III)–DTC species in solution. Finally, the complexes were screened for their antiproliferative activity against 2 human cancer cell lines, namely HepG2 and HepG2/SB3, taken as models of hepatocellular carcinoma. The latter, chosen for its aggressiveness due to the upregulation of the anti-apoptotic protein SerpinB3, was selectively inhibited in terms of growth by some Au(III)–DTC complexes.

Graphical abstract: Au(iii)-Proline derivatives exhibiting selective antiproliferative activity against HepG2/SB3 apoptosis-resistant cancer cells

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Publication details

The article was received on 24 Jul 2019, accepted on 24 Sep 2019 and first published on 27 Sep 2019


Article type: Paper
DOI: 10.1039/C9DT03036K
Dalton Trans., 2019, Advance Article

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    Au(III)-Proline derivatives exhibiting selective antiproliferative activity against HepG2/SB3 apoptosis-resistant cancer cells

    L. Brustolin, N. Pettenuzzo, C. Nardon, S. Quarta, L. Marchiò, B. Biondi, P. Pontisso and D. Fregona, Dalton Trans., 2019, Advance Article , DOI: 10.1039/C9DT03036K

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