Acridine-decorated cyclometallated gold(III) complexes: synthesis and anti-tumour investigations

被引:19
|
作者
Williams, Morwen R. M. [1 ]
Bertrand, Benoit [1 ,2 ]
Fernandez-Cestau, Julio [1 ]
Waller, Zoe A. E. [3 ]
O'Connell, Maria A. [3 ]
Searcey, Mark [1 ,3 ]
Bochmann, Manfred [1 ]
机构
[1] Univ East Anglia, Sch Chem, Norwich NR4 7TJ, Norfolk, England
[2] Sorbonne Univ, CNRS, IPCM, F-75005 Paris, France
[3] Univ East Anglia, Sch Pharm, Norwich NR4 7TJ, Norfolk, England
基金
欧洲研究理事会;
关键词
DNA-BINDING; CYTOTOXIC METALLODRUGS; BIOLOGICAL-PROPERTIES; TRANSPORT MECHANISMS; CRYSTAL-STRUCTURE; GOLD; LIGANDS; INHIBITION; PLATINUM; DERIVATIVES;
D O I
10.1039/c8dt02507j
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
(C boolean AND N) and (C boolean AND N boolean AND C) cyclometalated Au(iii) represent a highly promising class of potential anticancer agents. We report here the synthesis of seven new cyclometalated Au(iii) complexes with five of them bearing an acridine moiety attached via (N boolean AND O) or (N boolean AND N) chelates, acyclic amino carbenes (AAC) and N-heterocyclic carbenes (NHC). The antiproliferative properties of the different complexes were evaluated in vitro on a panel of cancer cells including leukaemia, lung and breast cancer cells. We observed a trend between the cytotoxicity and the intracellular gold uptake of some representative compounds of the series. Some of the acridine-decorated complexes were demonstrated to interact with ds-DNA using FRET-melting techniques.
引用
收藏
页码:13523 / 13534
页数:12
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