Article
Biochemistry & Molecular Biology
Najwa Mansour, Kikki Bodman-Smith, Rony S. Khnayzer, Costantine F. Daher
Summary: The photoactivatable Ru(II) complex 1 exhibited promising anticancer activity against triple negative adenocarcinoma MDA-MB-231 cells. Upon photoactivation, complex 1 showed time-dependent cytotoxic activity, inducing cell apoptosis and activating intrinsic and extrinsic pathways while inhibiting MAPK and PI3K pathways. The study suggests that complex 1 is a potent multimechanistic photoactivatable chemotherapeutic drug with potential for targeted cancer chemotherapy.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Biochemistry & Molecular Biology
Katia M. Oliveira, Joao Honorato, Felipe C. Demidoff, Mario S. Schultz, Chaquip D. Netto, Marcia R. Cominetti, Rodrigo S. Correa, Alzir A. Batista
Summary: The preparation and characterization of two new Ru(II)/diphosphine complexes containing Lapachol and Lawsone are described. These complexes exhibited high cytotoxicity against cancer cells, with complex (1) showing particular selectivity to triple-negative breast cancer cells. Mechanistic studies suggested that these complexes induce apoptosis in cancer cells through multiple pathways, making them promising candidates for cancer treatment.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Medicinal
Keyu Chen, Pan Li, Chunrong Zhu, Zhiyang Xia, Qian Xia, Lei Zhong, Bin Xiao, Tao Cheng, Changqiang Wu, Chengyi Shen, Xiaoming Zhang, Jiang Zhu
Summary: The novel Mn-BnO-TyrEDTA contrast agent improves the accuracy of liver lesion detection in MRI through hepatocyte uptake and renal clearance pathways, and achieves hepatic targeting through the organic anion transporting polypeptides (OATPs) mediated amphiphilic anion contrast agent uptake.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Sonia Infante-Tadeo, Vanessa Rodriguez-Fanjul, Cintia C. Vequi-Suplicy, Ana M. Pizarro
Summary: The passage describes the rapid hydrolysis and high basicity of complexes [Os(eta 6-arene)(C,N-phenylpyridine)Z] with chlorido or tethered oxygen as the ligand. It also reveals the structure-activity relationship between Os-CN and Os-NN complexes.
INORGANIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Hamid R. Shahsavari, Jiyun Hu, Samira Chamyani, Yoshie Sakamaki, Reza Babadi Aghakhanpour, Christopher Salmon, Masood Fereidoonnezhad, Ayyub Mojaddami, Parnian Peyvasteh, Hudson Beyzavi
Summary: Cationic cycloplatinated(II) complexes with bisphosphine ligands showed higher cytotoxicity compared to cisplatin across various cancer cell lines, especially complex 3 exhibiting excellent antiproliferative activity. The stability of these complexes in biological environments and their mode of interaction with DNA were also investigated.
Article
Chemistry, Inorganic & Nuclear
Stephen Mensah, Joseph D. Rosenthal, Mamta Dagar, Tyson Brown, Jonathan J. Mills, Christopher G. Hamaker, Gregory M. Ferrence, Michael I. Webb
Summary: The evolution of high virulence bacterial strains has led to the development of novel therapeutic agents. Metal-based therapeutics, with their structural variability and unique modes of action, show great promise. This study focused on the preparation and evaluation of ruthenium(ii)-arene complexes containing Schiff base ligands with an attached ferrocene, and identified a complex with prominent activity against clinically relevant bacterial strains.
DALTON TRANSACTIONS
(2022)
Review
Chemistry, Inorganic & Nuclear
Magdalena Malecka, Anna Skoczynska, David M. Goodman, Christian G. Hartinger, Elzbieta Budzisz
Summary: This review highlights the progress in the development of ruthenium(II)/(III) complexes with flavone derivatives as potential therapeutic agents, focusing on their antimicrobial, antitumor activity, and enzyme inhibition. The design concept for the Ru complexes as multitargeted compounds consisting of a bioactive ligand and a ruthenium center is also emphasized.
COORDINATION CHEMISTRY REVIEWS
(2021)
Article
Biochemistry & Molecular Biology
Maria George Elias, Stephanie Mehanna, Elias Elias, Rony S. Khnayzer, Costantine F. Daher
Summary: The study demonstrates that the photoactivated chemotherapy drug [Ru(bpy)2BC]Cl2 has multi-mechanistic effects, increasing cytotoxicity by inducing ROS production and DNA damage. It mediates apoptosis by interfering with pathways related to cell apoptosis.
CHEMICO-BIOLOGICAL INTERACTIONS
(2021)
Article
Chemistry, Multidisciplinary
Yuanwei Liang, Weiting Huang, Siqi Wang, Weiming Su, Qianyi Situ, Luxin He
Summary: In this study, a fairly small-sized aryl nitrogen mustard-conjugated terpyridine ligand was synthesized in only two steps to chelate with RuCl3 and form a [Ru(tpy-CM)(2)]Cl-2 complex. This complex showed prominent antiproliferative activity against several tumor cells, particularly human renal clear cell carcinoma cells, by inducing G1 phase cell cycle arrest and apoptosis.
JOURNAL OF CHEMICAL RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Zhu-Ying Yan, Jing Chen, Jie Shao, Ze-Qing Jiao, Tian-Shu Tang, Miao Tang, Zhi-Guo Sheng, Li Mao, Rong Huang, Chun-Hua Huang, Zhi-Hui Zhang, Hong-Mei Su, Ben-Zhan Zhu
Summary: The study identified a novel cell-impermeable Ru(II) polypyridyl cationic complex that generates high phototoxicity under visible light irradiation while demonstrating low dark toxicity, showing potential for applications in photodynamic therapy.
FREE RADICAL BIOLOGY AND MEDICINE
(2021)
Article
Chemistry, Multidisciplinary
Martin R. Gill, Paul J. Jarman, Vanessa Hearnden, Simon D. Fairbanks, Marcella Bassetto, John Palmer, Kathryn R. Ayscough, Jim A. Thomas, Carl Smythe
Summary: RuRuPhen blocks the transformation of G-actin monomers to F-actin filaments and disrupts the organization of actin stress fibers in cells. It interferes with actomyosin contractility, cell motility, and late-stage cytokinesis. RuRuPhen also interferes with the recruitment of endosomal sorting complexes required for transport (ESCRT) complex, leading to cytokinetic abscission failure.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Chemistry, Medicinal
Andrea Angeli, Mariana Pinteala, Stelian S. Maier, Alessandra Toti, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Silvia Selleri, Fabrizio Carta, Claudiu T. Supuran
Summary: This study evaluated the inhibitory effects of telluride-containing compounds on human carbonic anhydrase enzymes, with some compounds showing significant toxic effects against breast cancer cells. Under both normoxic and hypoxic conditions, these compounds demonstrated good efficacy in killing cancer cells.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Inorganic & Nuclear
Raphael T. Ryan, Dmytro Havrylyuk, Kimberly C. Stevens, L. Henry Moore, Sean Parkin, Jessica S. Blackburn, David K. Heidary, John P. Selegue, Edith C. Glazer
Summary: The beta-diketone scaffold, a commonly used synthetic intermediate, showed promising structure-dependent cytotoxicity in constructing Ru(II) complexes, suggesting the potential for future drug development.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Atousa Goudarzi, Mitra Ghassemzadeh, Maryam Saeidifar, Kioumars Aghapoor, Farshid Mohsenzadeh, Bernhard Neumueller
Summary: The synthesis of a new Pd(II) complex and its characterization were reported. The complex exhibited potent anticancer activity against MCF-7 breast cancer cells, and showed good antimicrobial activity against both Gram-positive and Gram-negative bacteria.
NEW JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Physical
Samah Akel, Malak A. Sharif, Razan Al-Esseili, Mohammad A. Al-Wahish, Hamdallah A. Hodali, Peter Mueller-Buschbaum, Lukas Schmidt-Mende, Mahmoud Al-Hussein
Summary: The study shows that a novel ruthenium complex can significantly improve the efficiency of ternary solar cells, with positive impacts on optical and morphological properties. However, increasing the concentration of the ruthenium complex leads to the formation of micron-size domains that negatively affect the optical properties and morphology of the active layer, diminishing the enhancement in device efficiency.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2021)
Article
Biochemistry & Molecular Biology
Lenka Markova, Vojtech Novohradsky, Jana Kasparkova, Jose Ruiz, Viktor Brabec
Summary: This study investigates the mechanism of the anticancer activity of a photoactivatable Ir(III) compound on highly aggressive and poorly treatable Rhabdomyosarcoma cells. The compound demonstrates potent activity in both differentiated cancer cells and cancer stem cells, and it affects mitochondrial function in a novel way. The findings suggest that this compound could be a promising chemotherapeutic agent for the treatment of hard-to-treat Rhabdomyosarcoma.
CHEMICO-BIOLOGICAL INTERACTIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Alicia Rey Planells, Arturo Espinosa Ferao
Summary: In this study, accurate ring strain energies (RSEs) for various inorganic and organic rings were computed using appropriate homodesmotic reactions. Special considerations were made for rings containing certain heteroatoms. The study also analyzed important concepts related to RSEs and proposed an alternative method for rapid estimation.
INORGANIC CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Jan Fassbender, Niklas Volk, Antonio Garcia Alcaraz, Selvakumar Balasubramaniam, Arturo Espinosa Ferao, Rainer Streubel
Summary: After more than 160 years of research, scientists have finally synthesized an oxaphosphirane, a phosphorus analogue derivative of oxirane. Reactions with various compounds have shown that increasing the coordination number at phosphorus causes destabilization, which supports previous findings. Theoretical studies have provided insights into ring strain energy, ring/ring interconversion, and oxidation pathways.
CHEMICAL COMMUNICATIONS
(2023)
Article
Chemistry, Applied
Miriam Mas-Montoya, Antonio Garcia Alcaraz, Arturo Espinosa Ferao, Delia Bautista, David Curiel
Summary: Two four-coordinate boron complexes, compounds 5 and 7, were synthesized using similar benzophenanthridine-based ligands but with different conformational constraints, and their optical properties were investigated. Ligand design considering expansion of pi-conjugation and structural desymmetrization was found to be effective in obtaining fluorophores with large Stokes shifts. The incorporation of a conformationally free substructure increased the geometry relaxation in the first excited state (S1) and the ground state (S0), resulting in enhanced Stokes shift. Solvatochromism showed divergent behavior in emission and absorption spectra, attributed to the different stabilization degrees of the S0 and S1 states compared to the Franck-Condon states. Aggregation-induced emission (AIE) was observed in molecule 7, which was attributed to blocking the motion of peripheral rotor based on solid state packing determined by X-ray diffraction.
Article
Chemistry, Applied
Francisco J. Ballester, Enrique Ortega-Forte, Delia Bautista, M. Dolores Santana, Giampaolo Barone, Jose Ruiz
Summary: In this study, a series of compounds with different substituents were synthesized and characterized using NMR and X-ray diffraction. It was found that compounds with stronger electron-donating groups exhibited larger Stokes shift and higher quantum yield. Additionally, some of the compounds showed higher activity in cancer cell lines while displaying low cytotoxicity in healthy cells. One of the compounds also showed the ability to stain the cytoplasm.
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
Anna Rovira, Enrique Ortega-Forte, Cormac Hally, Mireia Jorda-Redondo, Diego Abad-Montero, Gloria Vigueras, Jesus I. Martinez, Manel Bosch, Santi Nonell, Jose Ruiz, Vicente Marchan
Summary: Photodynamic therapy shows potential as a non-invasive anticancer tool, but the development of highly effective and non-toxic photosensitizers that can work under hypoxic conditions is still needed. In this study, Ir(III)-COUPY conjugates were developed based on the advantageous properties of COUPY fluorophores and cyclometalated Ir(III) complexes, aiming to explore structure-activity relationships. The structural modifications within the coumarin scaffold had a significant impact on the photophysical properties and cellular uptake of the conjugates. All Ir(III)-COUPY conjugates exhibited high phototoxicity under green light irradiation, attributed to the photogeneration of reactive oxygen species (ROS), while remaining non-toxic in the dark. Two hit conjugates showed excellent phototherapeutic indexes in cisplatin-resistant A2780cis cancer cells, indicating the potential of photoactive therapy approaches based on the conjugation of far-red/NIR-emitting COUPY dyes and transition metal complexes to overcome acquired resistance to cisplatin.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Arturo Espinosa Ferao, Alicia Rey Planells
Summary: Accurate ring strain energy (RSE) values were reported for sixty-six parent pnictogeniranes with two other identical p-block elements, El(2)Pn. A decrease in RSE was found to be correlated with an increase in the p character of the AO used in endocyclic bonds, particularly in groups 15 and 16. The higher -NICS(1) values also parallel the presence of atom-centred diatropic currents, mostly arising from the lone pairs. Only in the case of pnictogenaditrieliranes Tr(2)Pn (Tr=B, Al, Ga), the decrease of -NICS(1) is related to lower Huckel-type 2 pi-electron aromaticity in group 13.
CHEMISTRY-A EUROPEAN JOURNAL
(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, Multidisciplinary
Arturo Espinosa Ferao
Summary: This study explores the deoxygenation of parent and substituted oxiranes using lambda(3)sigma(3)-phosphorus reagents and reveals mechanistic aspects, as well as regio- and stereochemical consequences. It shows that attack to a ring C atom is usually preferred over direct P-to-O attack for one-step deoxygenation. The study also investigates the use of heavier derivatives AsMe3 and SbMe3 as oxirane deoxygenating reagents. The thermodynamic tendencies of lambda(3)sigma(3)-phosphorus reagents to act as oxygen or carbene acceptors are theoretically studied.
Article
Chemistry, Multidisciplinary
Enrique Ortega-Forte, Anna Rovira, Marta Lopez-Corrales, Alba Hernandez-Garcia, Francisco Jose Ballester, Eduardo Izquierdo-Garcia, Mireia Jorda-Redondo, Manel Bosch, Santi Nonell, Maria Dolores Santana, Jose Ruiz, Vicente Marchan, Gilles Gasser
Summary: Photodynamic therapy (PDT) is a promising cancer treatment method, but it is limited by its oxygen dependency and poor tissue penetration of some photosensitizers (PSs) activatable with short wavelengths. In this study, a novel hypoxia-active PS with operability in the near-infrared (NIR) region was developed, which showed high photoactivity toward cancer cells even under hypoxic environments. This strategy could potentially pave the way for the development of novel NIR- and hypoxia-active Ru(ii)-based theragnostic PSs.
Article
Chemistry, Inorganic & Nuclear
Alicia Marco, Gloria Vigueras, Natalia Busto, Natalia Cutillas, Delia Bautista, Jose Ruiz
Summary: New valproate Ir(iii) and Rh(iii) half-sandwich conjugates with a C,N-phenylbenzimidazole chelated ligand have been synthesized and characterized. The conjugation of valproic acid to organometallic fragments appears to enhance the antibacterial activity of the complexes against Enterococcus faecium and Staphylococcus aureus Gram-positive bacteria.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Inorganic & Nuclear
Arif Ali Khan, Tim Kalisch, Arturo Espinosa Ferao, Rainer Streubel
Summary: The reaction of a transient terminal phosphinidene complex with triethylamine resulted in the formation of an sp(3) C-H insertion product, as confirmed by P-31 NMR spectroscopy. The product was isolated as a semi-solid compound. However, after 24 hours of reaction, a primary phosphane complex was obtained. The compounds were characterized using NMR spectroscopy and mass spectrometry. Formation of the final products is explained by a mechanistic proposal based on DFT calculations.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Inorganic & Nuclear
Natalia Busto, Gloria Vigueras, Natalia Cutillas, Begona Garcia, Jose Ruiz
Summary: This study found that a new series of heteroleptic iridium(III) complexes showed remarkable effectiveness against Gram positive strains, especially Ir1 and Ir2, which were even 10 times more active than the fluoroquinolone antibiotic norfioxacin. The antimicrobial activity of these complexes is achieved by inducing ROS generation.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Joaquin Bonelli, Enrique Ortega-Forte, Gloria Vigueras, Manel Bosch, Natalia Cutillas, Josep Rocas, Jose Ruiz, Vicente Marchan
Summary: By encapsulating poorly soluble cyclometalated Ir(III) complexes using polyurethane-polyurea hybrid nanocapsules, their solubility is improved and the nanocapsules can enhance cellular uptake and cytotoxicity, leading to inhibition of tumor growth.
INORGANIC CHEMISTRY FRONTIERS
(2022)