Antiproliferative Activity of Gold(III) Complexes with Esters of Cyclohexyl-Functionalized Ethylenediamine-N,N’-Diacetate
Antiproliferative Activity of Gold(III) Complexes with Esters of Cyclohexyl-Functionalized Ethylenediamine-N,N’-Diacetate
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DOI：
10.1515/sjecr-2017-0067
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发表时间：
2013-11
影响因子：
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通讯作者：
N. Pantelić;T. Stanojković;B. B. Zmejkovski-B.;G. Kaluđerović;T. Sabo
中科院分区：
文献类型：
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作者：
N. Pantelić;T. Stanojković;B. B. Zmejkovski-B.;G. Kaluđerović;T. Sabo
合成了六种金（Ⅲ）与环己基官能化乙二胺-N，N '-二乙酸酯的配合物，通式为[AuCl 2 {（S，S）-R2 eddch}] PF 6，[（S，S）-eddch =（S，S）-乙二胺-N，N'-二-2-（3-环己基）丙酸酯，R分别= Me、Et、n-Pr、n-Bu、i-Bu、i-Am、1-6]，针对癌细胞系如人黑素瘤Fem-x，人结肠癌LS 174 T和非小细胞肺癌A549以及非癌性人胚胎肺成纤维细胞MRC-5，使用3-（4，5-二甲基噻唑-2-基）-2，5-二苯基溴化四唑（MTT）测定，目的是评估体外抗肿瘤活性和选择性。与用作参比化合物的顺铂相比，所有研究的复合物均显示出较低的细胞毒性和更好或相似的选择性。配合物[AuCl_2 {（S，S）-（i-Am）_2 eddch}] PF_6（6）对Fem-x的抑制活性最高（IC_（50）= 14.98 ± 0.34 μM）。此外，相同的复合物表达比顺铂高4.5倍的选择性。
Abstract Six gold(III) complexes with esters of cyclohexyl-functionalized ethylenediamine-N,N’-diacetate, general formula [AuCl2{(S,S)-R2eddch}]PF6, [(S,S)-eddch = (S,S)-ethylenediamine-N,N’-di-2-(3-cyclohexyl)propanoate, R = Me, Et, n-Pr, n-Bu, i-Bu, i-Am, 1–6, respectively], were tested against cancer cell lines such as human melanoma Fem-x, human colon carcinoma LS174T and non-small cell lung carcinoma A549 as well as a non-cancerous human embryonic lung fibroblasts MRC-5 using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay with the aim of assessing in vitro antitumoral activity and selectivity. All investigated complexes showed lower cytotoxicity and better or similar selectivity in comparison to cisplatin, used as reference compound. Complex [AuCl2{(S,S)-(i-Am)2eddch}]PF6 (6) demonstrated the highest activity against Fem-x (IC50 = 14.98 ± 0.34 μM). Additionally, the same complex expressed 4.5 times higher selectivity than cisplatin.