Pt(II) Rollover Cyclometalated Complexes Supported by 2,2’-Bipyridine N-Oxide: Synthesis, Characterization, and Biological Evaluation
Articolo
Data di Pubblicazione:
2026
Citazione:
Pt(II) Rollover Cyclometalated Complexes Supported by 2,2’-Bipyridine N-Oxide: Synthesis, Characterization, and Biological Evaluation / Zucca, A., Senzacqua, G., Canu, A., Ortu, F., Stoccoro, S., Pilo, M.I., Orrù, G., Pichiri, G., Fais, S., Scano, A.. - In: ORGANOMETALLICS. - ISSN 0276-7333. - (2026). [10.1021/acs.organomet.6c00114]
Abstract:
Four platinum(II) rollover cyclometalated complexes
derived from 2,2’-bipyridine N-oxide (bpyNO), [Pt(bpyNOH)(
DMSO)Me] (1a), [Pt(bpyNO-H)(PPh3)Me] (2a), [Pt(bpyNOH)(
DMSO)Cl] (3a), and [Pt(bpyNO-H)(PPh3)Cl] (4a), were
synthesized, characterized, and evaluated for their antimicrobial and
cytotoxic activities. The electron-poor nature of bpyNO enables
rollover C−H bond activation at room temperature. NMR and Xray
analysis (4a) revealed distinctive features, including an
intramolecular interaction between the H3′ hydrogen and the Noxide
oxygen. A correlation between the direct 195Pt−31P coupling
constant and the donating properties of cyclometalated ligands has
been found, allowing a useful scale of donor properties. A
preliminary screening of antimicrobial activity against E. coli, K.
pneumoniae, S. aureus multidrug resistant (MDR), S. pyogenes, P. aeruginosa, and C. albicans demonstrated selective activity. Complex
3a showed the most promising results against E. coli and multidrug-resistant S. aureus. Significantly, the complexes also exhibited
biofilm inhibitory behavior; notably, complex 1a showed activity against K. pneumoniae. Additionally, preliminary cytotoxicity tests
on human tumor (HT29) cells and normal (CCD 841 CoN) cells were performed. Among the investigated compounds, 1a, 2a, and
3a exhibited a significant reduction in tumor cell viability, whereas complex 4a displayed moderate activity. These results establish
2,2’-bipyridine N-oxide as a promising ligand scaffold for developing platinum complexes.
derived from 2,2’-bipyridine N-oxide (bpyNO), [Pt(bpyNOH)(
DMSO)Me] (1a), [Pt(bpyNO-H)(PPh3)Me] (2a), [Pt(bpyNOH)(
DMSO)Cl] (3a), and [Pt(bpyNO-H)(PPh3)Cl] (4a), were
synthesized, characterized, and evaluated for their antimicrobial and
cytotoxic activities. The electron-poor nature of bpyNO enables
rollover C−H bond activation at room temperature. NMR and Xray
analysis (4a) revealed distinctive features, including an
intramolecular interaction between the H3′ hydrogen and the Noxide
oxygen. A correlation between the direct 195Pt−31P coupling
constant and the donating properties of cyclometalated ligands has
been found, allowing a useful scale of donor properties. A
preliminary screening of antimicrobial activity against E. coli, K.
pneumoniae, S. aureus multidrug resistant (MDR), S. pyogenes, P. aeruginosa, and C. albicans demonstrated selective activity. Complex
3a showed the most promising results against E. coli and multidrug-resistant S. aureus. Significantly, the complexes also exhibited
biofilm inhibitory behavior; notably, complex 1a showed activity against K. pneumoniae. Additionally, preliminary cytotoxicity tests
on human tumor (HT29) cells and normal (CCD 841 CoN) cells were performed. Among the investigated compounds, 1a, 2a, and
3a exhibited a significant reduction in tumor cell viability, whereas complex 4a displayed moderate activity. These results establish
2,2’-bipyridine N-oxide as a promising ligand scaffold for developing platinum complexes.
Tipologia CRIS:
1.1 Articolo in rivista
Elenco autori:
Zucca, Antonio; Senzacqua, Giacomo; Canu, Antonio; Ortu, Fabrizio; Stoccoro, Sergio; Pilo, Maria I.; Orrù, Germano; Pichiri, Giuseppina; Fais, Sara; Scano, Alessandra
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