Cyclometalated (C^N^C)Au^III complexes bearing functionalized N‐heterocyclic carbene (NHC) ligands provide a high‐yielding, modular route to bioconjugated and binuclear complexes. This methodology has been applied to the synthesis of bioconjugated complexes presenting biotin and 17α‐ethynylestradiol vectors, as well as to the synthesis of bimetallic Au^III/Au^I complexes. The in vitro antiproliferative activities of these compounds against various cancer cells lines depend on the linker length, with the longer linker being the most potent. The estradiol conjugate AuC₆Estra proved to be more toxic against the estrogen receptor positive (ER+) cancer cells than against the ER− cancer cells and non‐cancer cells. The bimetallic complex AuC₆Au was more selective for breast cancer cells with respect to a healthy cell standard than the monometallic complex AuNHC. The metal uptake study on cells expressing or not biotin and estrogen receptors revealed an improved and targeted delivery of gold for both the bioconjugated complexes AuC₆Biot and AuC₆Estra compared to the non‐vectorised analogue AuNHC. The investigations of the interaction of the bioconjugates and bimetallic complexes with human telomeric G‐quadruplex DNA using FRET‐melting techniques revealed a reduced ability to stabilize this DNA structure with respect to the non‐vectorised analogue AuNHC.

中文翻译：

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合成双核和生物共轭复合物的金（III）钳配体支架：合成和抗癌潜力。

带有功能化N杂环卡宾（NHC）配体的环金属化（C ^ N ^ C）Au ^III配合物为生物共轭和双核配合物提供了高产量的模块化途径。该方法已应用于合成存在生物素和17α-乙炔基雌二醇载体的生物共轭复合物，以及双金属Au ^III / Au ^I复合物。这些化合物对各种癌细胞系的体外抗增殖活性取决于接头的长度，其中较长的接头是最有效的。雌二醇共轭AuC ₆ Estra被证明对雌激素受体阳性（ER +）癌细胞比对ER-癌细胞和非癌细胞具有更高的毒性。相对于健康细胞标准，双金属配合物AuC ₆ Au比单金属配合物AuNHC对乳腺癌细胞更具选择性。在表达或不生物素细胞和雌激素受体的摄取研究的金属揭示一种改进的和有针对性的金递送两者的生物共轭配合物的AuC ₆比奥和AuC中₆雌甾相对于非矢量化类似物AuNHC。使用FRET熔解技术对生物缀合物和双金属配合物与人类端粒G-四链体DNA相互作用的研究表明，与非载体化的类似物AuNHC相比，稳定这种DNA结构的能力降低了。