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Synthesis, characterization, and antitumor activity of unusual pseudo five coordinate gold(III) complexes: distinct cytotoxic mechanism or expensive ligand delivery systems?

Abstract：

:Gold(III) complexes bearing bidentate ligands based on the 1,10-phenanthroline and 2,2'-bipyridine scaffolds have shown promising anticancer activity against a variety of tumor cell lines. In particular, our laboratory has previously found that a pseudo five coordinate gold(III) complex possessing the 2,9-di-sec-butyl-1,10-phenanthroline ligand {[((di-sec-butyl)phen)AuCl3]} exhibits antitumor activity against a panel of five different lung and head-neck tumor cell lines. However, the [((di-sec-butyl)phen)AuCl3] complex was determined to be less active than the free 2,9-di-sec-butyl-1,10-phenanthroline ligand. In order to determine if this class of gold(III) complexes has a distinct mechanism of initiating tumor cell death or if these gold complexes simply release the polypyridyl ligand in the intracellular environment, structural analogues of the [((di-sec-butyl)phen)AuCl3] complex have been synthesized and structurally characterized. These structural congeners were prepared by using mono-alkyl and di-phenyl substituted 1,10-phenanthroline ligands, di-alkyl and di-phenyl substituted 4-methyl-1,10-phenanthroline ligands, and mono-alkyl 2,2'-bipyridine ligands. The redox stability of this library of distorted square pyramidal gold(III) complexes has been studied and the in vitro antitumor activity of gold(III) complexes and corresponding polypyridyl ligands has been determined. The [((di-n-butyl)phen)AuCl3] and [((mono-n-butyl)phen)AuCl3] complexes have been found to be significantly more potent at inhibiting the growth of A549 lung tumor cells than the clinically used drug cisplatin. More importantly, these two gold(III) complexes are significantly more active than their respective free ligands, providing evidence that this class of pseudo five coordinate gold(III) complexes has a mechanism of initiating tumor cell death that is independent of the free ligand.

journal_name

J Inorg Biochem

journal_title

Journal of inorganic biochemistry

authors

Olsen PM,Ruiz C,Lussier D,Le BK,Angel N,Smith M,Hwang CB,Khatib R,Jenkins J,Adams K,Getcher J,Tham F,Chen ZG,Wilson EH,Eichler JF

doi

10.1016/j.jinorgbio.2014.08.014

subject

Has Abstract

pub_date

2014-12-01 00:00:00

pages

121-131

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(14)00234-7

journal_volume

141

pub_type

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Synthesis, characterization, and antitumor activity of unusual pseudo five coordinate gold(III) complexes: distinct cytotoxic mechanism or expensive ligand delivery systems?