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首页> 外文期刊>Journal of Medicinal Chemistry >Gold(III) complexes as potential antitumor agents: solution chemistry and cytotoxic properties of some selected gold(III) compounds.
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Gold(III) complexes as potential antitumor agents: solution chemistry and cytotoxic properties of some selected gold(III) compounds.

机译：金（III）配合物作为潜在的抗肿瘤剂：某些选定的金（III）化合物的溶液化学和细胞毒性。

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Gold(III) complexes generally exhibit interesting cytotoxic and antitumor properties, but until now, their development has been heavily hampered by their poor stability under physiological conditions. To enhance the stability of the gold(III) center, we prepared a number of gold(III) complexes with multidentate ligands - namely [Au(en)(2)]Cl(3), [Au(dien)Cl]Cl(2), [Au(cyclam)](ClO(4))(2)Cl, [Au(terpy)Cl]Cl(2), and [Au(phen)Cl(2)]Cl - and analyzed their behavior in solution. The solution properties of these complexes were monitored by visible absorption spectroscopy, mass spectrometry, and chloride-selective potentiometric measurements; the electrochemical properties were also studied by cyclic voltammetry and coulometry. Since all the investigated compounds exhibited sufficient stability under physiological conditions, their cytotoxic properties were tested in vitro, via the sulforhodamine B assay, on the representative human ovarian tumor cell line A2780, either sensitive or resistant to cisplatin. In most cases the investigated compounds showed relevant cell-killing properties with IC(50) values falling in the 0.2-10 microM range; noticeably most investigated gold(III) complexes were able to overcome, to a large extent, resistance to cisplatin when tested on the corresponding cisplatin-resistant cell line. The cytotoxic properties of the free ligands were also determined under the same solution conditions. Ethylenediamine, diethylenetriamine, and cyclam were virtually nontoxic (IC(50) values > 100 microM) so that the relevant cytotoxic effects observed for [Au(en)(2)]Cl(3) and [Au(dien)Cl]Cl(2) could be quite unambiguously ascribed to the presence of the gold(III) center. In contrast the phenanthroline and terpyridine ligands turned out to be even more cytotoxic than the corresponding gold(III) complexes rendering the interpretation of the cytotoxicity profiles of the latter complexes less straightforward. The implications of the present findings for the development of novel gold(III) complexes as possible cytotoxic and antitumor drugs are discussed.
机译：金（III）配合物通常表现出令人感兴趣的细胞毒性和抗肿瘤特性，但是直到现在，由于其在生理条件下的稳定性差，它们的发展一直受到严重阻碍。为了增强金（III）中心的稳定性，我们制备了许多具有多齿配体的金（III）配合物-[Au（en）（2）] Cl（3），[Au（dien）Cl] Cl（ 2），[Au（cyclam）]（ClO（4））（2）Cl，[Au（terpy）Cl] Cl（2）和[Au（phen）Cl（2）] Cl-并分析了它们的行为解。这些配合物的溶液性质通过可见吸收光谱法，质谱法和氯离子选择性电位法进行监测。还通过循环伏安法和库仑法研究了电化学性能。由于所有研究的化合物在生理条件下均表现出足够的稳定性，因此通过磺基罗丹明B测定法在代表性的对顺铂敏感或耐药的人卵巢肿瘤细胞系A2780上体外测试了其细胞毒性。在大多数情况下，所研究的化合物显示出相关的细胞杀伤特性，IC（50）值在0.2-10 microM范围内。值得注意的是，在相应的顺铂耐药细胞系上进行测试时，大多数研究过的金（III）配合物都能在很大程度上克服对顺铂的耐药性。还在相同的溶液条件下测定了游离配体的细胞毒性。乙二胺，二亚乙基三胺和Cyclam实际上无毒（IC（50）值> 100 microM），因此观察到的有关[Au（en）（2）] Cl（3）和[Au（dien）Cl] Cl（ 2）可以明确地归因于金（III）中心的存在。相反，菲咯啉和三联吡啶配体被证明比相应的金（III）配合物更具细胞毒性，这使得后者配合物的细胞毒性谱的解释变得不那么直接。讨论了本研究结果对开发新型金（III）配合物作为可能的细胞毒性和抗肿瘤药物的意义。

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