Synthesis, characterization and cytotoxicity of new gold(III) complexes with 1,2-diaminocyclohexane: Influence of stereochemistry on antitumor activity
Synthesis, characterization and cytotoxicity of new gold(III) complexes with 1,2-diaminocyclohexane: Influence of stereochemistry on antitumor activity
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DOI：
10.1016/j.poly.2012.11.034
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发表时间：
2013-02-13
期刊：
影响因子：
2.6
通讯作者：
Altuwaijri, Saleh
中科院分区：
文献类型：
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作者：
Al-Jaroudi, Said S.;Fettouhi, Mohammed;Altuwaijri, Saleh
由四氯酸钠（III）二水合NaAuCl4中心点2H(2)O合成了[(DACH)AuCl2]Cl型金（III）配合物，其中DACH为二氨基环己烷。这些潜在的金属药物化合物使用各种光谱和分析技术进行了表征，包括元素分析、紫外可见光谱、红外光谱、溶液和固体核磁共振光谱以及x射线晶体学。通过远红外振动拉伸对Au-N键的稳定性、细胞毒性和胃癌细胞抑制作用等理化生化指标的测定，探讨了所合成的金（III）配合物作为抗癌药物的潜力。固体C-13核磁共振化学位移表明，配体通过N原子与金（III）中心强结合。配合物的x射线晶体学研究表明，环己基环呈椅状构象，金配位球呈扭曲的方形平面几何形状。溶液中顺式异构体对前列腺癌（PC-3）和胃癌（SGC-7901）等人癌细胞的抑制活性高于反式异构体。顺式异构体复合物在PC-3和SGC-7901细胞中的细胞毒性也被估计。(C) 2012 Elsevier Ltd.版权所有。
Gold(III) complexes of the type [(DACH)AuCl2]Cl, derived from sodium tetrachloroaurate(III) dihydrate NaAuCl4 center dot 2H(2)O, where DACH is diaminocyclohexane, have been synthesized. These potential metallodrug compounds were characterized using various spectroscopic and analytical techniques, including elemental analysis, UV-Vis, infrared spectroscopy, solution as well as solid NMR spectroscopy and X-ray crystallography. The potential of the synthesized gold(III) complexes as anti-cancer agents was investigated by measuring some relevant physicochemical and biochemical properties, such as the stability of the Au-N bonds by vibrational stretching from far-IR as well as cytotoxicity and the stomach cancer cell inhibiting effect. The solid-state C-13 NMR chemical shift shows that the ligand is strongly bound to the gold(III) center via N atoms. An X-ray crystallography study of the complexes shows that the cyclohexyl ring adopts a chair conformation and the gold coordination sphere adopts a distorted square planar geometry. The cis isomer in solution showed higher activity towards the inhibitory effect of human cancer cell lines such as prostate cancer (PC-3) and gastric carcinoma (SGC-7901) than that of the trans isomer. The cytotoxicity of the cis isomer complex has also been estimated in PC-3 and SGC-7901 cells. (C) 2012 Elsevier Ltd. All rights reserved.