Ni(II) Complexes of 2-Imine-8-Hydroxyquinolines: Characterization, Albumin Binding and Cytotoxicity
Abstract
Nickel(II) offers an appealing base for metallodrug design as it is abundant, inexpensive and forms well-defined complexes with N,O-donor ligands. Therefore, five Ni(II) complexes containing two tridentate 2-imine-8-hydroxyquinoline Schiff base ligands, derived from morpholine, piperidine, imidazole or 2-methyl-1H-limidazole, were synthesized and characterized in solution and solid state via analytical and spectroscopic techniques. Single crystals were solved using X-ray diffraction for the complex derived from 4-(2-aminopropyl)morpholine (1). This Ni(II) complex exhibits a distorted octahedrally coordinated Ni(II) center bound to two monodeprotonated NNO-tridentate ligands, adopting a meridional coordination mode, with the two oxygen atoms arranged cis to each other. The stability of the complexes in aqueous media buffered at pH 7.4 was evaluated with UV–Vis spectroscopy and their binding to bovine serum albumin (BSA) was assessed with fluorescence titrations. All complexes show strong reversible binding to BSA (KSV ~105), which stabilizes the lipophilic complexes in aqueous media. The antiproliferative activity of the complexes was screened against colon cancer cell lines (Colo205 and Colo320). They exhibit moderate anticancer activity (IC50 = 15.1–92.5 μM), with structure–activity relationships favoring imidazole derivatives and maintaining activity against the doxorubicin-resistant cell line (Colo320) with resistance indices (1.3–3.1) comparable to or lower than doxorubicin. Overall, the complexes represent a platform to develop new anticancer Ni-based drugs.
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BibTeX
@article{marcao2026niii,
title = {{Ni(II) Complexes of 2-Imine-8-Hydroxyquinolines: Characterization, Albumin Binding and Cytotoxicity}},
author = {Sofia Marcão and Leonor Côrte-Real and Alice Alborghetti and Maël Dejoux and Gabriella Spengler and Xavier Fontrodona and Isabel Romero and Éva A Enyedy and Alexandra M M Antunes and Isabel Correia},
journal = {Inorganics},
year = {2026},
month = sep,
doi = {10.3390/inorganics14090239},
url = {https://hal.science/hal-05847939v1},
note = {CC BY 4.0},
}
RIS
TY - JOUR
TI - Ni(II) Complexes of 2-Imine-8-Hydroxyquinolines: Characterization, Albumin Binding and Cytotoxicity
AU - Sofia Marcão
AU - Leonor Côrte-Real
AU - Alice Alborghetti
AU - Maël Dejoux
AU - Gabriella Spengler
AU - Xavier Fontrodona
AU - Isabel Romero
AU - Éva A Enyedy
AU - Alexandra M M Antunes
AU - Isabel Correia
PY - 2026
DA - 2026/09/10
JO - Inorganics
DO - 10.3390/inorganics14090239
UR - https://hal.science/hal-05847939v1
AB - Nickel(II) offers an appealing base for metallodrug design as it is abundant, inexpensive and forms well-defined complexes with N,O-donor ligands. Therefore, five Ni(II) complexes containing two tridentate 2-imine-8-hydroxyquinoline Schiff base ligands, derived from morpholine, piperidine, imidazole or 2-methyl-1H-limidazole, were synthesized and characterized in solution and solid state via analytical and spectroscopic techniques. Single crystals were solved using X-ray diffraction for the complex derived from 4-(2-aminopropyl)morpholine (1). This Ni(II) complex exhibits a distorted octahedrally coordinated Ni(II) center bound to two monodeprotonated NNO-tridentate ligands, adopting a meridional coordination mode, with the two oxygen atoms arranged cis to each other. The stability of the complexes in aqueous media buffered at pH 7.4 was evaluated with UV–Vis spectroscopy and their binding to bovine serum albumin (BSA) was assessed with fluorescence titrations. All complexes show strong reversible binding to BSA (KSV ~105), which stabilizes the lipophilic complexes in aqueous media. The antiproliferative activity of the complexes was screened against colon cancer cell lines (Colo205 and Colo320). They exhibit moderate anticancer activity (IC50 = 15.1–92.5 μM), with structure–activity relationships favoring imidazole derivatives and maintaining activity against the doxorubicin-resistant cell line (Colo320) with resistance indices (1.3–3.1) comparable to or lower than doxorubicin. Overall, the complexes represent a platform to develop new anticancer Ni-based drugs.
SN - 2304-6740
ER -