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Influence of the introduction of a triphenylphosphine group on the anticancer activity of a copper complex.

Abstract：

:Aiming at obtaining new copper complexes with good cytotoxicity against cancer cells, triphenylphosphine (TPP) was introduced to obtain insight into the influence of the co-ligands. In this paper, two copper complexes, Cu(2-pbmq)(CH3OH)Br2 (1) and [Cu(2-pbmq)(TPP)Br]2 (2) were designed, synthesized, and characterized by X-ray crystallography, 2-((2-(pyrazin-2-yl)-1H-benzo[d]imidazol-1-yl)methyl))quinolone (2-pbmq), to investigate the influence of the TPP group on the anticancer activity of the metal complex. Although the presence of the TPP group diminished the intensity of the interaction properties of the complex with DNA, the in vitro anticancer activity and cellular uptake of the TPP-containing complex were markedly superior to those of its TPP-lacking counterpart. Detailed studies on the more potently cytotoxic complex 2 revealed that it accumulated in nucleus, arrested the cell cycle at the G0-G1 phase, causing mitochondrial dysfunction, involving the potential simultaneous mitochondrial membrane collapse, cellular ATP level depletion, and Ca2+ leakage, eventually inducing cell apoptosis. In summary, the introduction of a TPP group enhances the biological activity and cytotoxicity of the complex.

journal_name

J Inorg Biochem

journal_title

Journal of inorganic biochemistry

authors

Li S,Zhao J,Guo Y,Mei Y,Yuan B,Gan N,Zhang J,Hu J,Hou H

doi

10.1016/j.jinorgbio.2020.111102

subject

Has Abstract

pub_date

2020-09-01 00:00:00

pages

111102

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(20)30130-6

journal_volume

210

pub_type

杂志文章

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