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Article

Synthesis, Antiproliferative Activity, and DNA Binding Studies of Nucleoamino Acid-Containing Pt(II) Complexes

1
Department of Chemical Sciences, University of Napoli Federico II, 80126 Napoli, Italy
2
CESTEV, University of Napoli Federico II, 80145 Napoli, Italy
3
CNR, Institute of Biostructure and Bioimaging, 80134 Napoli, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceuticals 2020, 13(10), 284; https://0-doi-org.brum.beds.ac.uk/10.3390/ph13100284
Received: 14 July 2020 / Revised: 25 September 2020 / Accepted: 28 September 2020 / Published: 30 September 2020
(This article belongs to the Special Issue Metal-Based Drugs: Updates and Perspectives)
We here report our studies on the reaction with the platinum(II) ion of a nucleoamino acid constituted by the l-2,3-diaminopropanoic acid linked to the thymine nucleobase through a methylenecarbonyl linker. The obtained new platinum complexes, characterized by spectroscopic and mass spectrometric techniques, were envisaged to exploit synergistic effects due to the presence of both the platinum center and the nucleoamino acid moiety. The latter can be potentially useful to protect the complexes from early deactivation, as well as to facilitate their cell internalization. The biological activity of the complexes in terms of antiproliferative effects was evaluated in vitro on different cancer cell lines and healthy cells, showing the best results on human cervical adenocarcinoma (HeLa) cells along with good selectivity for cancer over normal cells. In contrast, the metal-free nucleoamino acid did not show any cytotoxicity on both normal and cancer cell lines. Finally, the ability of the novel Pt(II) complexes to bind various DNA model systems was investigated by circular dichroism (CD) spectroscopy and polyacrylamide gel electrophoresis analyses proving that the newly obtained compounds can potentially target DNA, similarly to other well-known anticancer Pt complexes, with a peculiar G-quadruplex vs. duplex selectivity. View Full-Text
Keywords: Pt(II) complexes; nucleoamino acid ligand; NMR spectroscopy; antiproliferative activity; DNA binding studies; CD spectroscopy Pt(II) complexes; nucleoamino acid ligand; NMR spectroscopy; antiproliferative activity; DNA binding studies; CD spectroscopy
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MDPI and ACS Style

Riccardi, C.; Capasso, D.; Coppola, A.; Platella, C.; Montesarchio, D.; Di Gaetano, S.; Roviello, G.N.; Musumeci, D. Synthesis, Antiproliferative Activity, and DNA Binding Studies of Nucleoamino Acid-Containing Pt(II) Complexes. Pharmaceuticals 2020, 13, 284. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13100284

AMA Style

Riccardi C, Capasso D, Coppola A, Platella C, Montesarchio D, Di Gaetano S, Roviello GN, Musumeci D. Synthesis, Antiproliferative Activity, and DNA Binding Studies of Nucleoamino Acid-Containing Pt(II) Complexes. Pharmaceuticals. 2020; 13(10):284. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13100284

Chicago/Turabian Style

Riccardi, Claudia, Domenica Capasso, Angela Coppola, Chiara Platella, Daniela Montesarchio, Sonia Di Gaetano, Giovanni N. Roviello, and Domenica Musumeci. 2020. "Synthesis, Antiproliferative Activity, and DNA Binding Studies of Nucleoamino Acid-Containing Pt(II) Complexes" Pharmaceuticals 13, no. 10: 284. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13100284

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