Herein, we reported on the synthesis of a novel Pt(II) neutral complex having as ligand the nucleoside tubercidin, a potent anti-tumor agent extracted from the bacterium Streptomyces Tubercidicus. In detail, the chelation of the metal by a diamine linker installed at C6 purine position of tubercidin assured the introduction of a cisplatin-like unit in the molecular scaffold. The behavior of the synthesized complex with a double-strand DNA model was monitored by CD spectroscopy and compared with that of cisplatin and tubercidin. In addition, the cell viability was evaluated against HeLa, A375 and WM266 human cancer cell lines using the MTT test. Lastly, the results of the apoptotic assay (FITC Annexin V) performed on the HeLa cancer cell line are also reported.

Probing the DNA reactivity and the anticancer properties of a novel tubercidin-Pt(II) complex / D'Errico, S.; Falanga, A. P.; Capasso, D.; Gaetano, S. D.; Marzano, M.; Terracciano, M.; Roviello, G. N.; Piccialli, G.; Oliviero, G.; Borbone, N.. - In: PHARMACEUTICS. - ISSN 1999-4923. - 12:7(2020), pp. 1-16. [10.3390/pharmaceutics12070627]

Probing the DNA reactivity and the anticancer properties of a novel tubercidin-Pt(II) complex

D'errico S.
Primo
;
Falanga A. P.;Capasso D.;Marzano M.;Terracciano M.;Piccialli G.;Oliviero G.
;
Borbone N.
Ultimo
2020

Abstract

Herein, we reported on the synthesis of a novel Pt(II) neutral complex having as ligand the nucleoside tubercidin, a potent anti-tumor agent extracted from the bacterium Streptomyces Tubercidicus. In detail, the chelation of the metal by a diamine linker installed at C6 purine position of tubercidin assured the introduction of a cisplatin-like unit in the molecular scaffold. The behavior of the synthesized complex with a double-strand DNA model was monitored by CD spectroscopy and compared with that of cisplatin and tubercidin. In addition, the cell viability was evaluated against HeLa, A375 and WM266 human cancer cell lines using the MTT test. Lastly, the results of the apoptotic assay (FITC Annexin V) performed on the HeLa cancer cell line are also reported.
2020
Probing the DNA reactivity and the anticancer properties of a novel tubercidin-Pt(II) complex / D'Errico, S.; Falanga, A. P.; Capasso, D.; Gaetano, S. D.; Marzano, M.; Terracciano, M.; Roviello, G. N.; Piccialli, G.; Oliviero, G.; Borbone, N.. - In: PHARMACEUTICS. - ISSN 1999-4923. - 12:7(2020), pp. 1-16. [10.3390/pharmaceutics12070627]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/816767
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