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三价金配合物具有潜在的抗肿瘤活性,是目前金属药物领域的研究热点。本文按配位原子的不同总结了稳定三价金配合物的结构特征,按其生物活性的构效关系、生物靶点和作用机制综述了三价金配合物抗肿瘤活性研究的最新成果:配体的结构特点以及离去基团对三价金配合物的体外细胞毒性影响较大;介绍了用于检测三价金配合物与可能的生物靶分子之间相互作用的多种物理和生物学方法,重点关注了相互作用的模式,如嵌入/静电吸引/共价结合等,并解释了三价金配合物抗肿瘤活性的原因。最后提出了一些研究新思路,以期有助于设计得到靶标明确的具有良好药理活性的抗肿瘤药物。
Trivalent gold complexes have potential anti-tumor activity and are the hot topics in the field of metal drugs. This article summarizes the structural characteristics of the stable trivalent gold complexes by coordination atoms, and reviews the latest achievements in the study of the anti-tumor activity of trivalent gold complexes according to their structure-activity relationship, biological target and mechanism of action: The structural features of the body and the leaving group have a great influence on the in vitro cytotoxicity of the trivalent gold complex. Various physical and biological assays for detecting interactions between the trivalent gold complex and possible biological target molecules are introduced Method, with a focus on the modes of interaction such as intercalation / electrostatic attraction / covalent bonding, and explains the antitumor activity of the trivalent gold complex. Finally, some new research ideas are put forward in order to help design a well-targeted antitumor drug with good pharmacological activity.