An overview of advancement of organoruthenium(II) complexes as prospective anticancer agents

Bashir, Masrat; Mantoo, Imtiyaz Ahmad; Arjmand, Farukh; Tabassum, Sartaj; Yousuf, Imtiyaz

doi:10.1016/j.ccr.2023.215169

Cited by 31 publications

(8 citation statements)

References 147 publications

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“…Complexes 1-7 (except 4) are less cytotoxic to healthy MCF-10a and Vero cells than cisplatin, indicating that the general toxicity of this series of complexes is lower than that of cisplatin, and therefore more selective. This supports the collective hypothesis that is Ru-arene complexes usually exhibit lower general toxicity than cisplatin [37,38].…”

Section: Anticancer Activity Of Ru(ii)-arene Complexes 271 Mtt Cell P...supporting

confidence: 84%

Effective and Selective Ru(II)-Arene Complexes Containing 4,4′-Substituted 2,2′ Bipyridine Ligands Targeting Human Urinary Bladder Cancer Cells

Muralisankar

Chen

Haribabu

et al. 2023

IJMS

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Cisplatin-based chemotherapy is a common regimen for bladder cancer, a life-threatening cancer with more than 500,000 new cases worldwide annually. Like many other metallodrugs, cisplatin causes severe side effects for its general toxicity. Organoruthenium is known for its structural stability, good anticancer activity, and possible low general toxicity. Here, we have prepared and characterized a series of water-soluble ruthenium-arene complexes with N,N′-chelating ligands: [Ru(II)-η6-arene-(4,4′-(X)2-2,2′-bipyridine)Cl]Cl (arene = p-cymene, X = C4H9 (1), COOH (2), COOCH3 (3), COOC2H5 (4); arene = benzene, X = C4H9 (5), COOCH3 (6), COOC2H5 (7)). These complexes are carefully characterized using single-crystal X-ray diffraction, UV-vis, IR, 1H NMR, and MALDI-TOF MS spectroscopy. Their DFT-calculated structural and thermodynamic properties are consistent with the experimental observations. Biophysicochemical studies of complex interaction with CTDNA and BSA supported by molecular docking simulations reveal suitable properties of 1–7 as anticancer agents. Cytotoxicities of 1–7 are evaluated on healthy human MCF-10a-breast epithelial and African green monkey Vero cells, and carcinoma human HepG-2-hepatic, T24-bladder, and EAhy-926-endothelial cells. All complexes exhibit much higher cytotoxicity for T24 than cisplatin. Particularly, 1 and 2 are also highly selective toward T24. Fluorescence imaging and flow cytometry demonstrate that 1 and 2 penetrate T24 cell membrane and induce early apoptosis at their respective IC50 concentrations, which ultimately lead to cell death. Statistical analysis suggests that the order of importance for T24 cell antiproliferation is protein binding, Log p, Ru–Cl bond length, while DNA binding is the least important. This study is the first to report the anti-bladder cancer efficacy of Ru-arene-2,2′-bipyridine complexes, and may provide insights for rational design of organoruthenium drugs in the enduring search for new chemotherapeutic agents.

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Section: Anticancer Activity Of Ru(ii)-arene Complexes 271 Mtt Cell P...supporting

confidence: 84%

Effective and Selective Ru(II)-Arene Complexes Containing 4,4′-Substituted 2,2′ Bipyridine Ligands Targeting Human Urinary Bladder Cancer Cells

Muralisankar

Chen

Haribabu

et al. 2023

IJMS

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“…The therapeutic potential of Ru(II)-arene RAPTA-type compounds (PTA = 1,3,5-triaza-7-phosphaadamantane or 1,3,5-triaza-7-phosphatricyclo-[3.3.1.1]decanephosphine) has been thoroughly investigated, thus owing to the excellent antimetastatic property of the initial candidate RAPTA-C [Ru(η 6 -p-cymene)Cl 2 (PTA)] [119]. It is a multitargeting drug candidate that has demonstrated pH-dependent DNA damage, inhibited the enzyme activity of cathepsin-B and thioredoxin reductase, and showed selectivity towards the hypoxic environment of cancer cells [120]. It represents an innovative antitumor therapy and a better-tolerated alternative to Pt-based chemotherapeutic drugs in the treatment of tumors, as it exhibits antitumoral, antimetastatic, and antiangiogenic activities through protein and histone-deoxyribonucleic acid alterations [121].…”

Section: Rapta-cmentioning

confidence: 99%

Complexes of Ruthenium(II) as Promising Dual-Active Agents against Cancer and Viral Infections

D’Amato,

Mariconda,

Iacopetta

et al. 2023

Pharmaceuticals

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Poor responses to medical care and the failure of pharmacological treatment for many high-frequency diseases, such as cancer and viral infections, have been widely documented. In this context, numerous metal-based substances, including cisplatin, auranofin, various gold metallodrugs, and ruthenium complexes, are under study as possible anticancer and antiviral agents. The two Ru(III) and Ru(II) complexes, namely, BOLD-100 and RAPTA-C, are presently being studied in a clinical trial and preclinical studies evaluation, respectively, as anticancer agents. Interestingly, BOLD-100 has also recently demonstrated antiviral activity against SARS-CoV-2, which is the virus responsible for the COVID-19 pandemic. Over the last years, much effort has been dedicated to discovering new dual anticancer–antiviral agents. Ru-based complexes could be very suitable in this respect. Thus, this review focuses on the most recent studies regarding newly synthesized Ru(II) complexes for use as anticancer and/or antiviral agents.

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“…have been developed. 2–5 Among these complexes, cyclometalated neutral and cationic iridium( iii ) complexes with the general formula [(C^N) 2 Ir(XY)] 0/+ (neutral complex: XY = bidentate anionic ligand; cationic complex: XY = bidentate neutral ligand) were notable owing to their intrinsic luminescence properties, good cell permeability, interaction with some biomolecular targets and unique mechanisms of action (MoAs), which allowed for many applications such as bio-probes, cellular imaging reagents and highly active anticancer agents. 4,6–12 Most of these studies have been focused on the synthesis and biological evaluation of cyclometalated neutral and cationic complexes using different bidentate XY ligands, which have mostly been chosen as N^N donors (Scheme 1, I ).…”

Section: Introductionmentioning

confidence: 99%

Mitochondria-targeted neutral and cationic iridium(iii) anticancer complexes chelating simple hybrid sp²-N/sp³-N donor ligands

Li,

Guo,

et al. 2024

Dalton Trans.

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An overview of advancement of organoruthenium(II) complexes as prospective anticancer agents

Cited by 31 publications

References 147 publications

Effective and Selective Ru(II)-Arene Complexes Containing 4,4′-Substituted 2,2′ Bipyridine Ligands Targeting Human Urinary Bladder Cancer Cells

Effective and Selective Ru(II)-Arene Complexes Containing 4,4′-Substituted 2,2′ Bipyridine Ligands Targeting Human Urinary Bladder Cancer Cells

Complexes of Ruthenium(II) as Promising Dual-Active Agents against Cancer and Viral Infections

Mitochondria-targeted neutral and cationic iridium(iii) anticancer complexes chelating simple hybrid sp²-N/sp³-N donor ligands

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An overview of advancement of organoruthenium(II) complexes as prospective anticancer agents

Cited by 31 publications

References 147 publications

Effective and Selective Ru(II)-Arene Complexes Containing 4,4′-Substituted 2,2′ Bipyridine Ligands Targeting Human Urinary Bladder Cancer Cells

Effective and Selective Ru(II)-Arene Complexes Containing 4,4′-Substituted 2,2′ Bipyridine Ligands Targeting Human Urinary Bladder Cancer Cells

Complexes of Ruthenium(II) as Promising Dual-Active Agents against Cancer and Viral Infections

Mitochondria-targeted neutral and cationic iridium(iii) anticancer complexes chelating simple hybrid sp2-N/sp3-N donor ligands

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Mitochondria-targeted neutral and cationic iridium(iii) anticancer complexes chelating simple hybrid sp²-N/sp³-N donor ligands