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Review
. 2020 Dec 3:14:5375-5392.
doi: 10.2147/DDDT.S275007. eCollection 2020.

Ruthenium Complexes as Anticancer Agents: A Brief History and Perspectives

Sang Yeul Lee #  1 , Chul Young Kim #  1 , Tae-Gyu Nam  1
Affiliations
Review

Ruthenium Complexes as Anticancer Agents: A Brief History and Perspectives

Sang Yeul Lee et al. Drug Des Devel Ther. .

Abstract

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.

Keywords: metallo-anticancer; photoactivated chemotherapy; photodynamic therapy; ruthenium.

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Conflict of interest statement

The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
Ru complexes developed by Dwyer.
Figure 2
Figure 2
Approved Pt-based anticancer drugs.
Figure 3
Figure 3
Anticancer Ru complexes in clinical trials.
Figure 4
Figure 4
Selected RAPTA complexes from Ang and Dyson.
Figure 5
Figure 5
Selected anticancer RAPTA complexes.
Figure 6
Figure 6
Selected anticancer Ru polypyridyl complexes.
Figure 7
Figure 7
Selected Ru-based PDT agents.
Figure 8
Figure 8
Selected Ru-based PACT agents.
Figure 9
Figure 9
Crystal structure of the HAS-myristate-KP1019 complex. Two molecules of KP1019 bind to HAS at two histidine sites (H146 and H242).
Figure 10
Figure 10
Anticancer activity of NKP-1339. (A) Hep3B xenografts in Balb/c SCID mice was treated with NKP-1339 (30 mg/kg, iv, once a week) and/or sorafenib (25 mg/kg, po, five consecutive days per week) for two weeks. (B) The mechanisms underlying the anticancer activity of representative Ru complexes: KP1019 and NKP-1339.
See this image and copyright information in PMC

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