三价金配合物抗肿瘤活性研究*

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的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。

Antitumor Au(III) Complexes

Au(III) complexes have been extensively studied for their potential antitumor activity in the research of metallodrugs. In this paper, the stable Au(III) complexes are classified according to the coordination atoms and their characteristic structure. The recent development of the researches on the antitumor activity of Au(III) complexes including the structure-activity relationship, biological targets and the mechanisms of action are reviewed. The structure of the coordination ligand and the leaving group have great impact on the in vitro cytotoxicity of the Au(III) complex. Many physical and biological methods are introduced to study the interaction between the Au(III) complexes and the suspected bio-target, such as DNA, protein, mitochondrion, thio-containing biomolecules, etc. The interaction modes (intercalating, electrostatic interaction, covalent bonding, etc.) are focused to illustrate the reason for the antitumor activity of Au(III) complexes. Some new approaches are proposed for the designing and producing of a target-specific drug with a suitable pharmacological activity. Contents
1 Introduction
2 Structures of Au(III) complexes
2.1 N-coordinated Au(III) complexes
2.2 C-coordinated Au(III) complexes
2.3 {N,C}-coordinated Au(III) complexes
2.4 O/S/P/Se/Te-coordinated Au(III) complexes
2.5 Five/Six-coordinated Au(III) complexes
3 Antitumor activity of Au(III) complexes
3.1 Structure-activity relationship
3.2 Mechanism for the antitumor Au(III) complexes
4 Perspective of Au(III) complex
5 Conclusion