Article
Chemistry, Medicinal
Angelica E. Graminha, Cecilia Popolin, Joao Honorato de Araujo-Neto, Rodrigo S. Correa, Katia M. de Oliveira, Luani R. Godoy, Legna Colina Vegas, Javier Ellena, Alzir A. Batista, Marcia R. Cominetti
Summary: In this work, new ruthenium compounds with specific ligands were synthesized and characterized. The properties of these compounds in different solvents were studied, and their cytotoxicity against breast tumor cells and non-tumor cell lines was evaluated. One specific compound showed excellent selectivity towards the MDA-MB-231 cell line and induced apoptosis through the intrinsic pathway.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Pragti, Sreshtha Nayek, Satyam Singh, Avinash Sonawane, Ivo Grabchev, Rakesh Ganguly, Suman Mukhopadhyay
Summary: In this study, three Ru(II) arene complexes with a bidentate benzimidazole-based ligand were synthesized and their antitumor activity was studied by varying the co-ligand X. The synthesized compounds showed good interactions with serum albumin proteins, had good drug stability and lipophilic character. They were found to bind with DNA and could induce apoptosis in cancer cells, as well as upregulate cleaved caspase-3 expression and downregulate BCLXL expression. These findings provide a new direction for the investigation of antitumor ruthenium-based metallodrugs using benzimidazole-based ligands.
DALTON TRANSACTIONS
(2023)
Article
Pharmacology & Pharmacy
Desislava Budurova, Denitsa Momekova, Georgi Momekov, Pavletta Shestakova, Hristo Penchev, Stanislav Rangelov
Summary: This study explores the feasibility of using PEGylated calixarene as a carrier for silibinin, including the preparation and characterization of inclusion complexes and supramolecular aggregates, as well as dissolution tests. The results indicate that PEGylated calixarene, with the help of supramolecular aggregates, can significantly increase the water solubility of silibinin and exhibit good cytotoxicity against human tumor cell lines.
Article
Multidisciplinary Sciences
Patrick M. Perrigue, Agata Henschke, Bartosz F. Grzeskowiak, Lucja Przysiecka, Kaja Jaskot, Angelika Mielcarek, Emerson Coy, Sergio E. Moya
Summary: Understanding the interaction between nanoparticles and cells is crucial for designing more effective nanomedicines. This study investigates the biological fate of silica nanoparticles in senescent cells, which do not divide, using various methods including microscopy and flow cytometry. The results show that the nanoparticles readily enter the senescent cells and accumulate in the cytoplasm for a long time. This study lays the foundation for the development of NP-based tools for detecting and targeting senescent cells for therapeutic purposes.
SCIENTIFIC REPORTS
(2023)
Article
Chemistry, Applied
Rais Ahmad Khan, Amal AlFawaz, Nida N. Farshori, Anup Paul, Mohammed H. Jaafar, Ali Alsalme
Summary: Two organometallic ruthenium (II) complexes containing analogs of aminobenzimidazole were synthesized and characterized. Their binding affinity with human serum albumin and cytotoxic potential against cancer cells were evaluated. One of the complexes showed promising cytotoxic properties, indicating its potential as an anticancer therapeutic.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Roman O. Selin, Insa Klemt, Viktor Ya. Chernii, Mykhaylo Yu. Losytskyy, Svitlana Chernii, Andrzej Mular, Elzbieta Gumienna-Kontecka, Vladyslava B. Kovalska, Yan Z. Voloshin, Anna V. Vologzhanina, Pavel V. Dorovatovskii, Andriy Mokhir
Summary: A fluorescein-tagged iron(II) cage complex was obtained in moderate yield starting from its propargylamine-containing clathrochelate precursor. A significant decrease in fluorescence quantum yield was observed from the fluorescein-based dye to its clathrochelate derivative. The subcellular uptake of the fluorescein-tagged molecules mainly occurred in the cytosol, as visualized by fluorescence microscopy.
Article
Chemistry, Physical
Carley Giffert L. Nongpiur, Akalesh Kumar Verma, Mayur Mohan Ghate, Krishna Mohan Poluri, Werner Kaminsky, Mohan Rao Kollipara
Summary: We designed and synthesized a series of new structurally related Ru(II), Rh(III), and Ir(III) chelating complexes. The complexes were characterized by physicochemical and spectroscopic methods. The antibacterial and cytotoxic activities of the synthesized ligands and metal complexes were evaluated. The results showed that the metal complexes exhibited good antibacterial activity and act as potent anticancer agents.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Applied
Rais Ahmad Khan, Ibtisam I. BinSharfan, Seham S. Alterary, Huda Alsaeedi, Faizan Abul Qais, Amal AlFawaz, Arman D. Hadi, Ali Alsalme
Summary: The article presents the design and characterization of new ruthenium(II) p-cymene complexes with different ligands, as well as their interaction with human serum albumin. The cytotoxicity of these complexes against various cancer cells has been evaluated, showing promising results for potential use as anticancer metallodrugs.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Review
Chemistry, Inorganic & Nuclear
Daven Foster, S. M. Borhanuddin, Reto Dorta
Summary: Chiral ligands play a crucial role in asymmetric transition-metal catalysis, with N-heterocyclic carbenes (NHCs) exhibiting high levels of enantioselectivity. The field is expected to continue advancing in the future.
DALTON TRANSACTIONS
(2021)
Article
Chemistry, Multidisciplinary
Marzieh Dadkhah Aseman, Parisa Negaresh, Zahra Shojaeifard, Bahram Hemmateenejad, S. Masoud Nabavizadeh
Summary: The biomolecular interactions between two previously reported cycloplatinated complexes and bovine serum albumin (BSA) were investigated. The results showed a strong binding interaction between the complexes and the protein with a static quenching mechanism. The binding was found to be exothermic, involving mainly noncovalent hydrophobic forces and ionic interactions. The complexes induced structural changes in the protein and exhibited cytotoxicity against various cancer cell lines.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Satish S. Bhat, Vidyanand K. Revankar, Rahul V. Pinjari, Vijay Kumbar, Kishore Bhat, Vitthal A. Kawade
Summary: Two water-soluble ruthenium(II) polypyridyl complexes have been synthesized and characterized, and their structural, optical, and cellular imaging properties have been investigated. The complexes exhibit strong emission in aqueous solutions and show low toxicity towards human cancer and kidney cell lines. Fluorescence microscopy confirms their potential for cellular imaging applications.
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Chemistry, Multidisciplinary
Shaima Hkiri, Maxime Steinmetz, Rachel Schurhammer, David Semeril
Summary: This study successfully encapsulated a neutral complex inside a self-assembled hexameric capsule and confirmed the intra-cavity movements of the complex molecule, as well as possible supramolecular interactions with the aromatic rings of the capsule's inner part. The catalytic oxidation reaction showed different reaction kinetics for different substrates.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Biophysics
Monica Notarbartolo, Marina Massaro, Raquel de Melo Barbosa, Carlotta Emili, Leonarda Francesca Liotta, Paola Poma, Francisco M. Raymo, Rita Sanchez-Espejo, Riccardo Vago, Cesar Viseras-Iborra, Serena Riela
Summary: In recent years, there has been an increasing use of clay minerals in the pharmaceutical field. This study investigates the cellular uptake mechanisms of hectorite (Ht), a clay mineral with potential applications as a drug carrier. The study also explores the concept of covalently grafting the anticancer molecule methotrexate (MTX) onto Ht to form a nanomaterial. The results demonstrate the potential of Ht as a promising material for anticancer therapy.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2022)
Article
Chemistry, Inorganic & Nuclear
Ivelise Dimbarre Lao Guimaraes, Flavia Marszaukowski, Renan Ribeiro, Sergio Ricardo de Lazaro, Katia Mara de Oliveira, Alzir Azevedo Batista, Patricia Castellen, Ellen Wrobel, Jarem Raul Garcia, Rene T. Boere, Karen Wohnrath
Summary: Neutral Ru(II)-arene complexes with different ligands were synthesized, characterized, and evaluated for cytotoxicity against lung and breast cancer cell lines. The complexes showed varying solubility and cytotoxicity, with one complex displaying high cytotoxicity towards cancer cells but no activity against healthy cells, indicating some degree of selectivity.
JOURNAL OF ORGANOMETALLIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Giovanni Tabbi, Lorena Maria Cucci, Calogero Pinzino, Alessia Munzone, Tiziano Marzo, Silvia Pizzanelli, Cristina Satriano, Antonio Magri, Diego La Mendola
Summary: The study characterized copper complex species formed with peptide fragments derived from the N-terminal domain of the angiogenin protein. The amino group was identified as the main copper anchoring site for Ang1-17, with different coordination environments affecting the peptides' activity. Additionally, different protein isoforms showed varying effects on cellular copper uptake.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Inorganic & Nuclear
Alba Hernandez-Garcia, Lenka Markova, Maria Dolores Santana, Jitka Pracharova, Delia Bautista, Hana Kostrhunova, Vojtech Novohradsky, Viktor Brabec, Jose Ruiz, Jana Kasparkova
Summary: This study presents the synthesis and characterization of six new heteroleptic osmium(II) complexes with varying substituents in the R3 position of the phenyl ring of the cyclometalating C^N ligand. These complexes are highly kinetically inert and absorb a full-wavelength range of visible light. The antiproliferative activity of these complexes has been investigated using human cancer and noncancerous cell cultures, showing that they are more potent than conventional cisplatin. The mechanism of action involves the activation of the endoplasmic reticulum stress pathway and disruption of calcium homeostasis.
INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Hana Kostrhunova, Brondwyn S. McGhie, Lenka Markova, Olga Novakova, Jana Kasparkova, Janice R. Aldrich-Wright, Viktor Brabec
Summary: The platinum(II) complex Pt(II)56MeSS exhibits high potency against cancer cells but also displays side toxicity and in vivo activity. The synthesis of new platinum(IV) prodrugs combining Pt(II)56MeSS with diclofenac (DCF) is described. These Pt(IV) complexes show similar mechanisms of action as Pt(II)56MeSS and DCF, promoting antiproliferative activity and inducing cell death and immunogenic cell death in cancer cells.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Jaroslav Malina, Hana Kostrhunova, Peter Scott, Viktor Brabec
Summary: Fe(II)-based metallohelices were found to stabilize various DNA junctions, with the highest selectivity for the Y-shaped 3WJ. These metallohelices were shown to efficiently kill cancer cells and induce DNA damage, offering potential therapeutic benefits.
NUCLEIC ACIDS RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Amrita Sarkar, Vojtech Novohradsky, Moumita Maji, Tomer Babu, Lenka Markova, Hana Kostrhunova, Jana Kasparkova, Valentina Gandin, Viktor Brabec, Dan Gibson
Summary: A multitargeting prodrug (2) that releases gemcitabine, oxaliplatin, and doxorubicin in their active form in cancer cells is a potent cytotoxic agent. It selectively targets cancer cells with high selectivity indices and induces the release of DAMPs in CT26 cells. The prodrug also inhibits tumor growth in murine models with lower body weight loss compared to FDA drugs.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Medicinal
Vojtech Novohradsky, Alicia Marco, Lenka Markova, Natalia Cutillas, Jose Ruiz, Viktor Brabec
Summary: In this study, a series of new octahedral iridium(III) complexes Ir1-Ir9 were reported, which showed potential for inhibiting metastasis in triple-negative breast cancer. The results demonstrated that the structural modifications within the complexes strongly influenced their anti-metastatic properties, with complex Ir1 exhibiting the highest activity. Contrary to the effects of the conventional chemotherapy drug doxorubicin, which promoted metastatic properties of TNBC cells, the results suggested that doxorubicin therapy may increase the risk of breast cancer metastasis.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
J. P. C. Coverdale, H. Kostrhunova, L. Markova, H. Song, M. Postings, H. E. Bridgewater, V. Brabec, N. J. Rogers, P. Scott
Summary: Self-assembled enantiomers of a di-iron metallohelix showed different antiproliferative activities against HCT116 colon cancer cells, with the ?-helicity compound being more potent than the Delta compound. The accumulation and localization studies suggest that the ? enantiomer undergoes carrier-mediated efflux, while the Delta enantiomer undergoes equilibrative process. The binding of the ? metallohelix to DNA and inhibition of tubulin and actin networks contribute to its G(2)/M arrest effect on cells.
DALTON TRANSACTIONS
(2023)
Article
Biochemistry & Molecular Biology
Jitka Pracharova, Hana Kostrhunova, Alessandra Barbanente, Nicola Margiotta, Viktor Brabec
Summary: This study confirms the excellent antiproliferative activity of the phosphaplatin derivative RRD2 in various cancer cell lines and analyzes its binding to nuclear DNA. The results demonstrate that DNA lesions caused by RRD2 contribute to killing cancer cells. Additionally, RRD2 accumulates in cancer cells to a lesser extent than cisplatin but exhibits similar binding efficiency to nuclear DNA after accumulation.
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Jaroslav Malina, Hana Kostrhunova, Viktor Brabec
Summary: In this study, we investigated the interaction between a dinuclear nickel(II) tetracationic supramolecular helicate and DNA G-quadruplexes, and their impact on gene expression. The results showed that the supramolecular helicate preferentially binds to G-quadruplex structures and stabilizes them, leading to the inhibition of DNA synthesis and downregulation of gene expression.
INORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Biochemistry & Molecular Biology
Jana Kasparkova, Hana Kostrhunova, Vojtech Novohradsky, Lili Ma, Guangyu Zhu, Elena R. Milaeva, Alexender A. Shtill, Robin Vinck, Gilles Gasser, Viktor Brabec, Alexey A. Nazarov
Summary: This study investigated the mechanism of action of a Pt(IV) complex 2 with two axial lonidamine ligands, which selectively inhibit aerobic glycolysis. Compared to the parent Pt(II) complex, the presence of two lonidamine ligands increased the antiproliferative activity of complex 2, influenced its cell cycle profile and mechanism of cell death. In 3D cell culture, complex 2 exhibited exceptional antiproliferative activity.
Article
Chemistry, Inorganic & Nuclear
Vojtech Novohradsky, Lenka Markova, Hana Kostrhunova, Marie Svitelova, Jana Kasparkova, Alessandra Barbanente, Paride Papadia, Nicola Margiotta, James D. Hoeschele, Viktor Brabec
Summary: New platinum-based compounds exhibit high potency and selectivity in pancreatic cancer cells, and inhibit lipid synthesis through a novel mechanism, providing a potential theoretical basis for the development of new anticancer drugs.
INORGANIC CHEMISTRY FRONTIERS
(2022)