Review
Chemistry, Inorganic & Nuclear
Tasha R. Steel, Fearghal Walsh, Anna Wieczorek-Blauz, Muhammad Hanif, Christian G. Hartinger
Summary: Metallodrugs play a central role in the treatment and diagnosis of diseases, and the choice of ligands coordinated to the metal center is crucial for the biological activity of metal-based anticancer agents. Introducing bioactive ligands may lead to synergistic activity between the metal center and the ligand system, and Ru half-sandwich compounds are a promising class of anticancer agents that have been extensively studied.
COORDINATION CHEMISTRY REVIEWS
(2021)
Review
Chemistry, Inorganic & Nuclear
Masrat Bashir, Imtiyaz Ahmad Mantoo, Farukh Arjmand, Sartaj Tabassum, Imtiyaz Yousuf
Summary: The development of metal compounds as therapeutics and diagnostics drugs has increased due to the successful clinical use of platinum drugs for cancer treatment. Non-platinum anticancer agents, particularly ruthenium-based compounds, have emerged as promising alternatives due to their lower toxicity and ability to specifically accumulate and activate in tumor cells. Organoruthenium(II) complexes have attracted special attention because of their favorable biochemical properties and their dominant role in targeted chemotherapy. This review provides an overview of the latest advancements in developing organoruthenium(II) compounds as prospective anticancer agents and alternatives to platinum drugs, including their mechanisms of action, cytotoxic potential, and progress in clinical trials.
COORDINATION CHEMISTRY REVIEWS
(2023)
Article
Chemistry, Inorganic & Nuclear
Thi-Hien Dinh, Thi-Tam Trinh, Thi-Thu-Ha Phan, Hung-Huy Nguyen, Minh-Hai Nguyen
Summary: A series of alkali-lanthanide heterometallic complexes were prepared and structurally explored. The complexes exhibit different polymeric structures compared to the previously reported Na+-Ln3+ congeners. The morphology of Cs+-Ln3+ chains varies with the size of the rare earth ions. The Cs+ ions in the complexes with smaller rare earth ions show multiple interactions.
INORGANIC CHEMISTRY COMMUNICATIONS
(2023)
Review
Chemistry, Inorganic & Nuclear
William D. J. Tremlett, David M. Goodman, Tasha R. Steel, Saawan Kumar, Anna Wieczorek-Blauz, Fearghal P. Walsh, Matthew P. Sullivan, Muhammad Hanif, Christian G. Hartinger
Summary: The article discusses strategies to enhance the activity and reduce the side effects of metal-based drugs, as well as how these strategies can be applied to half-sandwich organoruthenium anticancer compounds.
COORDINATION CHEMISTRY REVIEWS
(2021)
Article
Biochemistry & Molecular Biology
Maria Azmanova, Laia Rafols, Patricia A. Cooper, Colin C. Seaton, Steven D. Shnyder, Anais Pitto-Barry
Summary: This study presents the synthesis, characterization, and evaluation of the in vitro cytotoxicity of five maleonitriledithiolate-based ruthenium metal complexes with various phosphine ligands. These complexes showed promising in vitro cytotoxicity against ovarian and lung cancer cell lines, as well as no toxicity in preliminary in vivo pilot studies. The mechanism of action suggests an apoptotic pathway based on ROS production.
Article
Chemistry, Inorganic & Nuclear
Lamia A. Ismail, Mohammad Y. Alfaifi, Serag Eldin Elbehairi, Reda F. M. Elshaarawy, Emad M. Gad, W. N. El-Sayed
Summary: Two new hybrid half-sandwiched Ru(II) arene complexes have been synthesized, showing significant inhibitory activity against human breast and lung cancer cells with lower micromolar IC50 values. The complexes exhibit intercalative modes of interaction with DNA and a preference for binding to complex 4b. These new hybrid organoruthenium(II) complexes may offer promising safe anticancer agents, with no activity against normal cell lines.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Peter A. Ajibade, Amos A. Fatokun, Athandwe M. Paca
Summary: In this study, a new organoruthenium(II) complex was synthesized and characterized. The complex exhibits a centrosymmetric binuclear structure and shows potent cytotoxicity against cervical and lung cancer cell lines. The compound outperformed cisplatin in terms of cytotoxic potency, highlighting its potential as an anti-cancer agent.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Engineering, Electrical & Electronic
Anjli Hooda, Devender Singh, Kapeesha Nehra, Anuj Dalal, Sumit Kumar, Rajender Singh Malik, Vikas Siwach, Parvin Kumar
Summary: Mononuclear Sm(III) complexes with luminous and conducting behavior were synthesized using fluorinated organic chromophoric moiety and heteroaromatic Lewis bases. Spectroscopic analysis showed that diketone and coligand were attached to Sm(III) metal ion via oxygen (-O) and nitrogen (-N) donor atom, respectively. The optical and electronic band gap data suggested the conducting character of the complexes. The absorption patterns exhibited broad bands, and upon UV irradiation, the emission patterns showed characteristic peaks in the visible region. The CIE color coordinates confirmed the luminescent nature of the complexes in the orange-red region, indicating their potential in producing optoelectronic materials.
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN ELECTRONICS
(2023)
Article
Chemistry, Physical
Vladislav V. Krisyuk, Samara Urkasym Kyzy, Aleksandr S. Sukhikh, Asiya E. Turgambaeva
Summary: New lithium complexes with fluorinated and non-fluorinated methoxy-substituted, beta-diketonates were prepared and their crystal structures were determined by X-ray analysis. Thermal properties investigation showed that these complexes are volatile and sublime upon heating.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Inorganic & Nuclear
Chezhiyan Sumithaa, Przemyslaw Gajda-Morszewski, Wickneswaran Ishaniya, Themmila Khamrang, Marappan Velusamy, Nattamai Bhuvanesh, Malgorzata Brindell, Olga Mazuryk, Mani Ganeshpandian
Summary: Despite extensive research on metallodrugs and nanocarriers, there is a lack of strategies to optimize the design of both in a concerted effort. This study evaluates three ruthenium complexes as potential anticancer candidates and designs polydiacetylene-coated mesoporous silica nanoparticles as a functional nanocarrier. The complexes show promising cytotoxicity, with Ru(pyr) exhibiting the highest potency, while the nanocarriers enhance drug release and cellular internalization. The results suggest the potential application of these nanocarriers for in vivo investigations.
DALTON TRANSACTIONS
(2023)
Article
Biochemistry & Molecular Biology
Vladislav V. Krisyuk, Samara Urkasym Kyzy, Tatyana V. Rybalova, Ilya V. Korolkov, Mariya A. Grebenkina, Alexander N. Lavrov
Summary: The possibility of obtaining volatile heterometallic complexes containing lanthanides and transition metals bound by methoxy-beta-diketonates was studied. New compounds were prepared by cocrystallization of monometallic complexes from organic solvents. The thermal properties of the complexes were investigated by TG-DTA and vacuum sublimation tests. The heterometallic complexes were found to be not volatile and decomposed under heating to produce inorganic composites, while the monometallic complexes showed volatility and could be sublimed in a vacuum.
Article
Biochemistry & Molecular Biology
Evgeniia S. Vikulova, Taisiya S. Sukhikh, Sergey A. Gulyaev, Igor Yu. Ilyin, Natalia B. Morozova
Summary: This research examines the role of fluorination and solvents in the structural organization of Ag(I) coordination polymers. Through the synthesis of various compounds, the study demonstrates that the choice of solvent can lead to different structural types of chain coordination polymers.
Article
Chemistry, Applied
Kristina Mihajlovic, Nenad Joksimovic, Jelena Petronijevic, Ignjat Filipovic, Nenad Jankovic, Emilija Milovic, Suzana Popovic, Sanja Matic, Dejan Baskic
Summary: This study tested a series of beta-diketonate compounds for their cytotoxicity and selectivity against tumor cells and normal cells, and investigated their interactions with biomacromolecules. The results showed that these compounds have great potential for application.
NATURAL PRODUCT RESEARCH
(2023)
Article
Chemistry, Inorganic & Nuclear
Maura Pellei, Jo Del Gobbo, Miriam Caviglia, Deepika V. V. Karade, Valentina Gandin, Cristina Marzano, Anurag Noonikara Poyil, H. V. Rasika Dias, Carlo Santini
Summary: The design, synthesis, and in vitro antitumor properties of Cu(i) and Ag(i) phosphane complexes supported by the anions of sterically hindered β-diketone ligands have been reported. The copper(i) and silver(i) complexes of the parent ligand were also synthesized and included in the study. These metal complexes exhibit significant antitumor properties and are more potent than cisplatin in inhibiting cancer cell growth.
DALTON TRANSACTIONS
(2023)
Article
Biochemistry & Molecular Biology
Katherine D. Bauman, Vikram V. Shende, Percival Yang-Ting Chen, Daniela B. B. Trivella, Tobias A. M. Gulder, Sreekumar Vellalath, Daniel Romo, Bradley S. Moore
Summary: This study reports an enzymatic route to the salinosporamide core and reveals the catalytic role of a ketosynthase, SalC, in transacylation and bond-forming reactions. The crystal structure of SalC and site-directed mutagenesis studies proposed a bicyclization reaction mechanism. This work challenges our understanding of ketosynthase enzymes and provides a foundation for the streamlined production of clinically relevant chemotherapeutics in the future.
NATURE CHEMICAL BIOLOGY
(2022)
Article
Pharmacology & Pharmacy
Dina Baier, Beatrix Schoenhacker-Alte, Mate Rusz, Christine Pirker, Thomas Mohr, Theresa Mendrina, Dominik Kirchhofer, Samuel M. Meier-Menches, Katharina Hohenwallner, Martin Schaier, Evelyn Rampler, Gunda Koellensperger, Petra Heffeter, Bernhard Keppler, Walter Berger
Summary: Cellular energy metabolism is reprogrammed in cancer cells, leading to resistance against ruthenium-based chemotherapy drug BOLD-100 through enhanced glycolytic activity, increased lysosomal compartment, and defective downstream autophagy execution. Combining 2-deoxy-D-glucose with BOLD-100 reverses this resistance by inducing synergistic cell death and disrupting autophagy, suggesting glycolysis as a potential target to enhance BOLD-100 anticancer activity.
Article
Pharmacology & Pharmacy
Alexandra Kostelidou, Franc Perdih, Jakob Kljun, Foteini Dimou, Stavros Kalogiannis, Iztok Turel, George Psomas
Summary: A series of complexes of divalent transition metals with the quinolone antibacterial agent fleroxacin were prepared and characterized. The complexes showed higher antibacterial activity than free quinolone and exhibited tight binding to serum albumin and DNA.
Article
Biochemistry & Molecular Biology
Marko Novinec, Primoz Bembic, Milica Jankovic, Marija Kisilak, Jakob Kljun, Iztok Turel
Summary: Heavy metal ions, such as gallium and cerium, can inhibit the activity of human papain-like cysteine endopeptidases, while zinc and lead ions are known inhibitors of thiol enzymes. The inhibition constants of Ga3+, Ce3+, and Ce4+ ions are comparable to Zn2+ ions, indicating their potential as cysteine cathepsin inhibitors. These ions also inhibit the degradation of elastin, suggesting their possible application in treating inflammatory diseases.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Tomaz Trobec, Monika C. Zuzek, Kristina Sepcic, Jerneja Kladnik, Iztok Turel, Robert Frangez
Summary: Butyrylcholinesterase (BChE) is a therapeutic target for Alzheimer's disease. The organoruthenium(II) complex C1 was designed to selectively inhibit horse serum BChE. C1 showed no significant effect on nerve-evoked contractions but decreased the amplitude of miniature end-plate potentials (MEPP) and shortened the half-decay time of MEPPs and end-plate potentials (EPP). The results suggest a weak inhibitory effect on muscle-type nicotinic acetylcholine receptors (nAChR), but do not significantly affect neuromuscular transmission and skeletal muscle contraction.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Tina P. Andrejevic, Ivana Aleksic, Jakob Kljun, Marta Pockaj, Matija Zlatar, Sandra Vojnovic, Jasmina Nikodinovic-Runic, Iztok Turel, Milos I. Djuran, Biljana D. Glisic
Summary: Dimethyl 6-(pyrazine-2-yl)pyridine-3,4-dicarboxylate (py-2pz) was used as a ligand to synthesize new copper(II) and silver(I) complexes. The structures of the complexes were determined by single crystal X-ray diffraction analysis, revealing the bidentate coordination mode of py-2pz to the metal ions. Silver(I) complexes showed good antimicrobial activity against bacteria and fungi. The binding affinity of the complexes with DNA and protein was studied to understand their antimicrobial mechanism. The copper(II) complexes exhibited biomimetic catalytic activity.
Article
Biochemistry & Molecular Biology
Jakob Kljun, Mihaela Rebernik, Lucia M. Balsa, Jerneja Kladnik, Uros Rapus, Tomaz Trobec, Kristina Sepcic, Robert Frangez, Ignacio E. Leon, Iztok Turel
Summary: Organoruthenium pyrithione complexes, such as [(eta(6)-p-cymene)Ru(pyrithionato)(pta)]PF6, show promise as a new class of anticancer drugs. Our study focuses on finding alternatives to the pta ligand and discovering new structural elements to improve the biological properties of ruthenium anticancer drugs. By replacing the pta ligand with different phosphine, phosphite, and arsine ligands, we identified improved inhibitory potency against the enzyme glutathione S-transferase, as well as investigated cytotoxicity in breast, bone, and colon cancers.
Article
Pharmacology & Pharmacy
Yvonne Lerchbammer-Kreith, Michaela Hejl, Petra Vician, Michael A. Jakupec, Walter Berger, Mathea S. Galanski, Bernhard K. Keppler
Summary: Based on their drug delivery properties and activity against tumors, PAMAM dendrimers were combined with platinum(IV) complexes to improve anticancer treatment. The conjugates showed faster reduction behavior compared to the platinum(IV) complexes and exhibited significantly increased cytotoxic activity in human cell lines. In vivo experiments demonstrated tumor growth inhibition and prolonged animal survival.
Article
Pharmacology & Pharmacy
Rostyslav Panchuk, Nadiya Skorokhyd, Vira Chumak, Lilya Lehka, Halyna Kosiakova, Tetyana Horid'ko, Iehor Hudz, Nadiya Hula, Anna Riabtseva, Nataliya Mitina, Alexander Zaichenko, Petra Heffeter, Walter Berger, Rostyslav Stoika
Summary: This study discovered the pro-apoptotic effects of synthetic cannabimimetic N-stearoylethanolamine (NSE) on various cancer cell lines, including drug-resistant models. The study also synthesized a complex of NSE with a polymeric carrier, which enhanced the anticancer activity of doxorubicin and prevented its adverse effects in mice. Overall, the novel pharmaceutical formulation of NSE showed bi-functionality by promoting apoptosis in cancer cells and enhancing the therapeutic activity of doxorubicin while minimizing side effects.
Article
Chemistry, Multidisciplinary
Martin Schaier, Sarah Theiner, Dina Baier, Gabriel Braun, Walter Berger, Gunda Koellensperger
Summary: In this study, a workflow combining low-dispersion laser ablation with inductively coupled plasma time-of-flight mass spectrometry (LA-ICP-TOFMS) was presented, enabling spatial single-cell metallomics in tissue to decode cellular heterogeneity. The toolbox of single-cell metallomics was expanded by integrating the concepts of imaging mass cytometry (IMC) to utilize metal-labeled antibodies for cellular tissue profiling.
Article
Cell Biology
Livia Gruber, Maximilian Jobst, Endre Kiss, Martina Karasova, Bernhard Englinger, Walter Berger, Giorgia Del Favero
Summary: Bladder cells rely on the cytoskeletal network and endoplasmic reticulum (ER) to maintain mechanical stability. The rearrangement of ER can lead to changes in cellular mechanical properties.
CELL COMMUNICATION AND SIGNALING
(2023)
Article
Chemistry, Multidisciplinary
Andrea Geri, Lara Massai, Marko Novinec, Iztok Turel, Luigi Messori
Summary: Medicinal gold compounds exert their pharmacological effects by binding to protein targets. In this study, the reactions between seven representative gold compounds and the cysteine protease cathepsin B were explored, revealing strong interactions with the free cysteine in the enzyme. The findings suggest that the chemical nature of the gold compound plays a significant role in its interaction with proteins.
Article
Cell Biology
Alexander Ries, Astrid Slany, Christine Pirker, Johanna C. C. Mader, Doris Mejri, Thomas Mohr, Karin Schelch, Daniela Flehberger, Nadine Maach, Muhammad Hashim, Mir Alireza Hoda, Balazs Dome, Georg Krupitza, Walter Berger, Christopher Gerner, Klaus Holzmann, Michael Grusch
Summary: In this study, novel hTERT-transduced mesothelial cell and Meso-CAF models were generated and characterized, and their impact on PM cell growth was investigated.
Article
Chemistry, Inorganic & Nuclear
Alexander Kastner, Theresa Mendrina, Florian Bachmann, Walter Berger, Bernhard K. Keppler, Petra Heffeter, Christian R. Kowol
Summary: In this study, oxaliplatin(iv)-based complexes were developed as platinum(iv) prodrugs to release aspirin, which has shown antitumor activity against colon cancer. The newly synthesized complex demonstrated increased reduction stability compared to a cisplatin analog and exhibited desired prodrug properties in cell culture. A derivative with albumin-binding properties showed improved pharmacokinetics and tumor accumulation, leading to enhanced antitumor activity and overall survival in tumor-bearing mice.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Correction
Biochemistry & Molecular Biology
Jerneja Kladnik, Ana Dolinar, Jakob Kljun, David Perea, Judith Grau-Exposito, Meritxell Genesca, Marko Novinec, Maria J. Buzon, Iztok Turel
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
