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Cancers 2019, 11(4), 474; https://doi.org/10.3390/cancers11040474

Potent In Vitro and In Vivo Anticancer Activity of New Bipyridine and Bipyrimidine Gold (III) Dithiocarbamate Derivatives

1
Department of Chemistry, GC University, Lahore 54000, Pakistan
2
Molecular Oncology, Centro di Riferimento Oncologico di Aviano (CRO) IRCCS, 33081 Aviano, Italy
3
Department of Chemistry, King Fahd University of Petroleum and Minerals, Dhahran 31261, Saudi Arabia
4
Immunopathology and Cancer Biomarkers, Centro di Riferimento Oncologico di Aviano (CRO) IRCCS, 33081 Aviano, Italy
5
Center for Technological Transfer, Edmund Mach Foundation, 38010 Trento, Italy
6
Lab Technical Support Office (LTSO), King Fahd University of Petroleum and Minerals, Dhahran 31261, Saudi Arabia
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Received: 12 February 2019 / Revised: 12 March 2019 / Accepted: 18 March 2019 / Published: 4 April 2019
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Abstract

We synthesized eight new bipyridine and bipyrimidine gold (III) dithiocarbamate-containing complexes (C1C8) and tested them in a panel of human cancer cell lines. We used osteosarcoma (MG-63), lung (A549), prostate (PC3 and DU145), breast (MCF-7), ovarian (A2780 and A2780cis, cisplatin- and doxorubicin-resistant), and cervical (ME-180 and R-ME-180, cisplatin resistant) cancer cell lines. We found that C2, C3, C6, and C7 were more cytotoxic than cisplatin in all cell lines tested and overcame cisplatin and doxorubicin resistance in A2780cis and R-ME-180 cells. In the PC3 prostate cancer cell line, the gold (III) complex C6 ([Au2(BPM)(DMDTC)2]Cl4) induced apoptosis and double-stranded DNA breaks, modified cell cycle phases, increased Reactive Oxigen Species (ROS) generation, and reduced thioredoxin reductase and proteasome activities. It inhibited PC3 cell migration and was more cytotoxic against PC3 cells than normal human adipose-derived stromal cells. In mice bearing PC3 tumor xenografts, C6 reduced tumor growth by more than 70% without causing weight loss. Altogether, our results demonstrate the anticancer activity of these new gold (III) complexes and support the potential of C6 as a new agent for prostate cancer treatment. View Full-Text
Keywords: gold (III) complexes; anticancer therapy; cisplatin resistance; doxorubicin resistance; prostate cancer gold (III) complexes; anticancer therapy; cisplatin resistance; doxorubicin resistance; prostate cancer
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Altaf, M.; Casagrande, N.; Mariotto, E.; Baig, N.; Kawde, A.-N.; Corona, G.; Larcher, R.; Borghese, C.; Pavan, C.; Seliman, A.A.; Aldinucci, D.; Isab, A.A. Potent In Vitro and In Vivo Anticancer Activity of New Bipyridine and Bipyrimidine Gold (III) Dithiocarbamate Derivatives. Cancers 2019, 11, 474.

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