Abstract Platinum iodido complexes have long been recognized as synthetic intermediates of various platinum complexes (e.g., chlorido or carboxylato), including the world-wide used platinum-based anticancer drugs cisplatin, carboplatin and oxaliplatin. At the same time, platinum iodido complexes have been overlooked by bioinorganic chemists, because several pioneer works deemed the iodido ligand as unsuitable for the development of novel platinum-based metallotherapeutics. This was because most of platinum iodido complexes were identified as biologically and pharmacologically non-prospective as compared with the chlorido analogues. More recently, several research teams have developed various types of platinum iodido complexes as substances possessing the combination of promising chemical, physical, and especially biological properties. In particular, a number of platinum iodido complexes showed higher activity than their chlorido analogues and they exceeded even the activity of the conventional platinum-based drugs. Additionally, a lot of results have implied that relevant differences exist in the mechanism of action between platinum iodido agents, and their chlorido analogues and clinically-used platinum complexes. Herein, we offer a comprehensive overview of anticancer active platinum iodido complexes, together with the most relevant aspects of their mechanisms of action. We focused on all the structural types, differing in the platinum oxidation state, nuclearity, number of iodido ligands and type/s of donor atoms of the non-iodido ligands involved in the inner coordination sphere. The profound differences in the mechanisms of interactions of platinum(II) iodido complexes with biomolecules have been identified in contrast to the clinically used platinum-based metallotherapeutics. The platinum(IV) diiodido complexes represent the inactive prodrugs photoactivable to the active platinum(II) species. In addition, a number of organometallic and multinuclear platinum iodido complexes were identified among the most active agents. The reviewed platinum iodido complexes offer such unique features that they might fuel the design of novel, highly active, more specific and safer potential platinum-based therapeutics.

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碘化铂络合物：抗癌活性和作用机制的综合概述

摘要 碘化铂络合物长期以来一直被认为是各种铂络合物（如氯代或羧基）的合成中间体，包括世界广泛使用的铂类抗癌药物顺铂、卡铂和奥沙利铂。同时，碘化铂络合物已被生物无机化学家忽视，因为一些先驱工作认为碘化配体不适合开发新型铂基金属治疗剂。这是因为与氯化物类似物相比，大多数碘化铂络合物被确定为在生物学和药理学上没有前瞻性。最近，几个研究小组开发了各种类型的碘化铂络合物，作为具有有前途的化学、物理，尤其是生物学特性的物质。特别是，一些碘化铂络合物的活性高于其氯化物类似物，甚至超过了传统铂类药物的活性。此外，大量研究结果表明，碘化铂类药物及其氯化物类似物和临床使用的铂类配合物的作用机制存在相关差异。在此，我们全面概述了具有抗癌活性的碘化铂络合物，以及它们作用机制的最相关方面。我们专注于所有结构类型，在铂氧化态、核度、碘配体数量和参与内部配位层的非碘配体的供体原子类型方面有所不同。与临床上使用的铂类金属治疗药物相比，已发现铂 (II) 碘配合物与生物分子的相互作用机制存在巨大差异。铂 (IV) 二碘络合物代表对活性铂 (II) 物质可光活化的非活性前药。此外，一些有机金属和多核碘化铂络合物被确定为最活跃的试剂。所审查的碘化铂络合物具有如此独特的特性，它们可能会推动新型、高活性、更具体和更安全的潜在铂基疗法的设计。铂 (IV) 二碘络合物代表对活性铂 (II) 物质可光活化的非活性前药。此外，一些有机金属和多核碘化铂络合物被确定为最活跃的试剂。所审查的碘化铂络合物具有如此独特的特性，它们可能会推动新型、高活性、更具体和更安全的潜在铂基疗法的设计。铂 (IV) 二碘络合物代表对活性铂 (II) 物质可光活化的非活性前药。此外，一些有机金属和多核碘化铂络合物被确定为最活跃的试剂。所审查的碘化铂络合物具有如此独特的特性，它们可能会推动新型、高活性、更具体和更安全的潜在铂基疗法的设计。