Aiming toward compounds with improved anti-
activity by exploiting the parasite auxotrophies, a library of nucleobase-tethered trithiolato-bridged dinuclear ruthenium(II)-arene conjugates was ...synthesized and evaluated. Structural features such as the type of nucleobase and linking unit were progressively modified. For comparison, diruthenium hybrids with other type of molecules were also synthesized and assessed. A total of 37 compounds (diruthenium conjugates and intermediates) were evaluated in a primary screening for in vitro activity against transgenic
tachyzoites constitutively expressing β-galactosidase (
β-gal) at 0.1 and 1 µM. In parallel, the cytotoxicity in non-infected host cells (human foreskin fibroblasts, HFF) was determined by alamarBlue assay. Twenty compounds strongly impairing parasite proliferation with little effect on HFF viability were subjected to
β-gal half maximal inhibitory concentration determination (IC
) and their toxicity for HFF was assessed at 2.5 µM. Two promising compounds were identified:
, ester conjugate with 9-(2-oxyethyl)adenine, and
, a click conjugate bearing a 2-(4-(hydroxymethyl)-1
-1,2,3-triazol-1-yl)methyl substituent, with IC
values of 0.059 and 0.111 µM respectively, significantly lower compared to pyrimethamine standard (IC
= 0.326 µM). Both
and
exhibited low toxicity against HFF when applied at 2.5 µM and are candidates for potential treatment options in a suitable in vivo model.
The stereoselective preparation of synthetically versatile vinylboronates from ω-alkenylboronates is achieved through a ruthenium-catalyzed isomerization reaction. A variety of di- and trisubstituted ...vinylboronates were conveniently produced and could be used as a new starting point for subsequent in situ remote functionalization through either a sequential Ru/Pd or Ru/Cu double catalytic system.
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Ruthenium compounds have become promising alternatives to platinum drugs by displaying specific activities against different cancers and favorable toxicity and clearance properties. ...Here, we show that the ruthenium(II) complex Ru(p-cymene)(bis(3,5-dimethylpyrazol-1-yl)methane)ClCl (UNICAM-1) exhibits potent in vivo antitumor effects. When administered as four-dose course, by repeating a single dose (52.4mgkg-1) every three days, UNICAM-1 significantly reduces the growth of A17 triple negative breast cancer cells transplanted into FVB syngeneic mice. Pharmacokinetic studies indicate that UNICAM-1 is rapidly eliminated from kidney, liver and bloodstream thanks to its high hydrosolubility, exerting excellent therapeutic activity with minimal side effects. Immunohistological analysis revealed that the efficacy of UNICAM-1, mainly relies on its capacity to reverse tumor-associated immune suppression by significantly reducing the number of tumor-infiltrating regulatory T cells. Therefore, UNICAM-1 appears very promising for the treatment of TNBC.
Ruthenium complexes have attracted considerable interest as potential antitumor agents. Therefore, antitumor activity and systemic toxicity of ruthenium(II) terpyridine complexes were evaluated in ...heterotopic mouse colon carcinoma. In the present study, cytotoxic effects of recently synthesized ruthenium(II) terpyridine complexes Ru(Cl-tpy)(en)ClCl (en = ethylenediamine, tpy = terpyridine,
) and Ru(Cl-tpy)(dach)ClCl (dach = 1,2-diaminocyclohexane,
) towards human and murine colon carcinoma cells were tested in vitro and in vivo and compared with oxaliplatin, the most commonly used chemotherapeutic agent against colorectal carcinoma. Ruthenium(II) complexes showed moderate cytotoxicity with IC
values ranging between 19.1 to 167.3 μM against two human, HCT116 and SW480, and one mouse colon carcinoma cell line, CT26. Both ruthenium(II) terpyridine complexes exerted a moderate apoptotic effect in colon carcinoma cells, but induced significant necrotic death. Additionally, both complexes induced cell cycle disturbances, but these effects were specific for the cell line. Further,
significantly reduced the growth of primary heterotopic tumor in mice, similarly to oxaliplatin. Renal damage in
treated mice was lower in comparison with oxaliplatin treated mice, as evaluated by serum levels of urea and creatinine and histological evaluation, but
induced higher liver damage than oxaliplatin, evaluated by the serum levels of alanine aminotransferase. Additionally, the interaction of these ruthenium(II) terpyridine complexes with the tripeptide glutathione (GSH) was investigated by proton nuclear magnetic resonance (
H NMR) spectroscopy. All reactions led to the formation of monofunctional thiolate adducts Ru(Cl-tpy)(en)GS-
(
) and Ru(Cl-tpy)(dach)GS-
(
). Our data highlight the significant cytotoxic activity of Ru(Cl-tpy)(en)ClCl against human and mouse colon carcinoma cells, as well as in vivo antitumor activity in CT26 tumor-bearing mice similar to standard chemotherapeutic oxaliplatin, accompanied with lower nephrotoxicity in comparison with oxaliplatin.
Dye sensitized solar cell (DSSC) is one of the most capable solar cell devices to transform sunlight directly into electricity. DSSC can revolutionize the solar energy industry due to its unique ...features and has attracted a lot of attention towards this alternative solar cell technology. DSSC can be manufactured with low-cost materials, easy manufacturing methods, less toxic materials, and most important, allocating feasibility of solar cell fabrication at a low cost as compared to traditional solar cells. The NREL certified power conversion efficiency (PCE) for DSSC is 12.3%, whereas the lab-scale PCE has reached 14.3%. In this paper, we present an introduction and classification of PV technologies and a brief description of DSSC development particularly ruthenium complexes based DSSC. This review also presents the structure, operational principle of DSSC and includes the essential criteria for the components of DSSC to offer a vision for the design of highly efficient DSSC. The research progress made in sensitizers especially in ruthenium complexes based have been summarized with their efficiency, dye structure, short circuit current (Isc), open circuit voltage (Voc) and fill factor (FF).
Ruthenium‐catalyzed C−H chalcogenations of anilides with readily available diselenides and disulfides have been achieved. Our strategy features ample substrate scope, affording the mono‐ortho ...selenylated and thiolated anilides with complete site selectivity control and high catalytic efficacy. Detailed mechanistic studies provide strong support for a facile base‐assisted internal electrophilic substitution (BIES) metalation event.
Conventional development of nanomaterials for efficient electrocatalysis is largely based on performance‐oriented trial‐and‐error/iterative approaches, while a rational design approach at the ...atomic/molecular level is yet to be found. Here, inspired by a fundamental understanding of the mechanism for both oxygen and hydrogen evolution half reactions (OER/HER), a unique strategy is presented to engineer RuO2 for superior alkaline water electrolysis through coupling with NiO as an efficient bifunctional promoter. Benefitting from desired potential‐induced interfacial synergies, NiO‐derived NiOOH improves the oxygen binding energy of RuO2 for enhanced OER, and NiO also promotes water dissociation for enhanced HER on RuO2‐derived Ru. The resulting hybrid material exhibits remarkable bifunctional activities, affording 2.6 times higher OER activity than that of RuO2 and an HER activity comparable to Pt/C. As a result, the simple system requires only 1.5 V to deliver 10 mA cm−2 for overall alkaline water splitting, outperforming the benchmark PtC/NF||IrO2/NF couple with high mass loading. Comprehensive electrochemical investigation reveals the unique and critical role of NiO on the optimized RuO2/NiO interface for synergistically enhanced activities, which may be extended to broader (electro)catalytic systems.
Porous nanosheet arrays consisting of strongly interacting RuO2 and NiO nanoparticles are grown vertically on nickel foam through a simple hydrothermal reaction, chemical etching, and thermal treatment process. The self‐supported electrode performs as a highly efficient bifunctional electrocatalyst for overall alkaline water splitting. Its enhanced activity is largely due to the potential‐induced interfacial synergy originating from its rational design.
Hybrid capacitor materials exhibit good electrochemical performance because they possess the advantages of both electrical double-layer capacitors (EDLCs) and pseudocapacitors (PCs). Here, ruthenium ...nanohybrid compounds (Ru-com) are synthesized with hydrous ruthenium oxide (RuO2·H2O), EDLCs, and ruthenium nanoparticles capped by cysteine (Ru-cys), which are PCs. The morphologies and structures of Ru-com, RuO2·H2O, and Ru-cys are confirmed by several characterization methods. The electrochemical performances are investigated by cyclic voltammetry, galvanostatic charging-discharging, and electrochemical impedance spectroscopy. The Ru-com exhibits a specific capacitance of 797.7 A g−1 in 0.5 M H2SO4 electrolyte at a scan rate of 10 mV s−1, which is much larger than the specific capacitance of its precursors, due to the synergistic effect of the reversible faradaic redox process and facilitated proton and electron transfer processes. In addition, the Ru-com not only shows a better rate capability than Ru-cys but also exhibits a better electrochemical stability than RuO2·H2O owing to the mutual modification of its components.
•Ru based hybrid nanocompounds with both RuIV and Ru0 part were synthesized.•Ru-com shows greatly improved specific capacitance of 797.7 F g−1.•Ru-com has the merits of electrical double-layer capacitors and pseudocapacitors.
Inducing necroptosis in cancer cells is an effective approach to circumvent drug‐resistance. Metal‐based triggers have, however, rarely been reported. Ruthenium(II) complexes containing ...1,1‐(pyrazin‐2‐yl)pyreno4,5‐e1,2,4triazine were developed with a series of different ancillary ligands (Ru1‐7). The combination of the main ligand with bipyridyl and phenylpyridyl ligands endows Ru7 with superior nucleus‐targeting properties. As a rare dual catalytic inhibitor, Ru7 effectively inhibits the endogenous activities of topoisomerase (topo) I and II and kills cancer cells by necroptosis. The cell signaling pathway from topo inhibition to necroptosis was elucidated. Furthermore, Ru7 displays significant antitumor activity against drug‐resistant cancer cells in vivo. To the best of our knowledge, Ru7 is the first Ru‐based necroptosis‐inducing chemotherapeutic agent.
RuII complexes were developed to act as dual catalytic inhibitors of topoisomerase I and II. Tuning of the auxiliary ligands gave complex Ru7, which targets the nucleus of cancer cells effectively, inducing cell death via necroptosis. The cell signaling pathways were investigated and the in vivo activity against drug resistant cancer was found to be excellent.
A heterogeneous ruthenium catalyst consisting of isolated single atoms and disordered clusters stabilized in a N-doped carbon matrix has been synthesized with very good activity and remarkable ...regioselectivity in the hydroformylation of 1-hexene. The role of the nitrogen heteroatoms has been probed essential to increase the catalyst stability and activity, enabling the stabilization of Ru(II)–N sites according to X-ray photoelectron spectroscopy (XPS) and XANES. Intrinsic size-dependent activity of Ru species of different atomicity has been extracted, correlating the observed reaction rate and the particle size distribution determined by means of aberration-corrected high-angle annular dark-field scanning transmission electron microscopy, permitting the identification of single-atom sites as the most active ones. This catalyst appears as a promising alternative with respect to its heterogeneous counterparts, paving the way for designing improved Ru heterogeneous catalysts.
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