Department of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Gyeonggi-do 15588, Republic of Korea.
Drug Des Devel Ther. 2020 Dec 3;14:5375-5392. doi: 10.2147/DDDT.S275007. eCollection 2020.
Platinum (Pt)-based anticancer drugs such as cisplatin have been used to treat various cancers. However, they have some limitations including poor selectivity and toxicity towards normal cells and increasing chemoresistance. Therefore, there is a need for novel metallo-anticancers, which has not been met for decades. Since the initial introduction of ruthenium (Ru) polypyridyl complex, a number of attempts at structural evolution have been conducted to improve efficacy. Among them, half-sandwich Ru-arene complexes have been the most prominent as an anticancer platform. Such complexes have clearly shown superior anticancer profiles such as increased selectivity toward cancer cells and ameliorating toxicity against normal cells compared to existing Pt-based anticancers. Currently, several Ru complexes are under human clinical trials. For improvement in selectivity and toxicity associated with chemotherapy, Ru complexes as photodynamic therapy (PDT), and photoactivated chemotherapy (PACT), which can selectively activate prodrug moieties in a specific region, have also been investigated. With all these studies on these interesting entities, new metallo-anticancer drugs to at least partially replace existing Pt-based anticancers are anticipated. This review covers a brief description of Ru-based anticancer complexes and perspectives.
铂（Pt）类抗癌药物如顺铂已被用于治疗各种癌症。然而，它们存在一些局限性，包括对正常细胞的选择性差和毒性增加以及化学耐药性的增加。因此，需要新型的金属抗癌药物，但几十年来一直没有得到满足。自最初引入钌（Ru）多吡啶配合物以来，已经进行了许多结构演化的尝试，以提高功效。其中，半夹心 Ru-芳烃配合物作为抗癌平台最为突出。与现有的基于 Pt 的抗癌药物相比，这些配合物明显显示出更好的抗癌特性，例如对癌细胞的选择性增加和对正常细胞的毒性降低。目前，有几种 Ru 复合物正在进行人体临床试验。为了提高与化疗相关的选择性和毒性，Ru 复合物作为光动力疗法（PDT）和光激活化疗（PACT）也得到了研究，这些方法可以在特定区域选择性地激活前药部分。随着对这些有趣实体的所有这些研究，预计至少有部分替代现有基于 Pt 的抗癌药物的新型金属抗癌药物将会出现。本综述简要介绍了基于 Ru 的抗癌配合物及其前景。
