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.

Title 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.
Authors M. Litecká; M. Hreusová; J. Ka?párková; R. Gyepes; R. Smolková; J. Obuch; T. David; I. Poto??ák
Journal Bioorg Med Chem Lett
DOI 10.1016/j.bmcl.2020.127206
Abstract

Four gallium(III) complexes, [Ga(ClQ)]?MeOH (1 - MeOH), [Ga(ClQ)] (1), [Ga(BrQ)] (2), [Ga(dIQ)] (3) and [Ga(CQ)] (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 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 values in the range 2.1-6 ?m) compared to the ClQ ligand and cisplatin; and a significant selective antiproliferative potency (IC = 136 ?m, 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.

Citation M. Litecká; M. Hreusová; J. Ka?párková; R. Gyepes; R. Smolková; J. Obuch; T. David; I. Poto??ák.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.. Bioorg Med Chem Lett. 2020;30(13):127206. doi:10.1016/j.bmcl.2020.127206

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Gallium

See more Gallium products. Gallium (atomic symbol: Ga, atomic number: 31) is a Block P, Group 13, Period 4 element with an atomic weight of 69.723.The number of electrons in each of Gallium's shells is 2, 8, 18, 3 and its electron configuration is [Ar] 3d10 4s2 4p1. The gallium atom has a radius of 122.1 pm and a Van der Waals radius of 187 pm. Gallium Bohr ModelGallium was predicted by Dmitri Mendeleev in 1871. It was first discovered and isolated by Lecoq de Boisbaudran in 1875. In its elemental form, gallium has a silvery appearance. Elemental GalliumGallium is one of three elements that occur naturally as a liquid at room temperature, the other two being mercury and cesium. Gallium does not exist as a free element in nature and is sourced commercially from bauxite and sphalerite. Currently, gallium is used in semiconductor devices for microelectronics and optics. The element name originates from the Latin word 'Gallia' referring to Gaul, the old name of France.

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