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Low-dimensional compounds containing bioactive ligands. Part XIV: High selective antiproliferative activity of tris(5-chloro-8-quinolinolato)gallium (III) complex against human cancer cell lines

Publication at Faculty of Science, Central Library of Charles University |
2020

Abstract

Four gallium(III) complexes, [Ga(ClQ)(3)]·MeOH (1 - MeOH), [Ga(ClQ)(3)] (1), [Ga(BrQ)(3)] (2), [Ga(dIQ)(3)] (3) and [Ga(CQ)(3)] (4), were prepared (H-ClQ = 5-chloro-8-quinolinol, H-BrQ = 7-bromo-8-quinolinol, H-dIQ = 5,7-diiodo-8-quinolinol, H-CQ = 5-chloro-7-iodo-8-quinolinol) and characterised by elemental analysis, IR and NMR spectroscopy. Single crystal structure analysis of 1 - MeOH confirmed that the complex has a molecular structure with gallium(III) metal ion coordinated in mer-fashion by N- and O-donor atoms of three ClQ ligands.

Stability of all complexes in DMSO was proved by (1)H NMR spectroscopy. The in vitro antiproliferative activity of 1 was evaluated against the A2780, MBA-MB-231 and HCT116 cell lines.

Complex 1 displays higher antiproliferative activity (IC(50) values in the range 2.1-6 μM) compared to the ClQ ligand and cisplatin; and a significant selective antiproliferative potency (IC(50) = 136 μM, for normal MRC5pd30 cell line). Radical scavenging experiments revealed that complex 1 exhibits the highest antioxidant activity of the prepared complexes as well as the ligands.