Article
Pharmacology & Pharmacy
Si'an Fang, Yuhao Jiang, Di Xiao, Xuran Zhang, Qianqian Gan, Qing Ruan, Junbo Zhang
Summary: By synthesizing and labeling novel norfloxacin isonitrile derivatives CN4NF and CN5NF, it was found that [Tc-99m]Tc-CN5NF showed high specificity to bacteria, could differentiate bacterial infection from sterile inflammation in vivo, and had the potential to be a radiotracer for bacterial infection imaging.
Article
Biochemistry & Molecular Biology
Christos Kiritsis, Antonio Shegani, Konstantina Makrypidi, Ioanna Roupa, Aristotelis Lazopoulos, Angeliki Panagiotopoulou, Sotiria Triantopoulou, Maria Paravatou-Petsotas, Hans-Juergen Pietzsch, Maria Pelecanou, Minas Papadopoulos, Ioannis Pirmettis
Summary: The synthesis, characterization, and biological evaluation of new 4 + 1 mixed-ligand Re-III- and Tc-99m(III)-complexes have shown promising activity in inhibiting cell growth and potential efficacy in EGFR autophosphorylation studies.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Analytical
Maximilian Horstmann, Melanie Austrup, Felix Busch, Andreas Faust, Michael Sperling, Uwe Karst, David Clases
Summary: A speciation analysis method combining liquid chromatography with elemental and molecular mass spectrometry is developed to directly identify, characterize, and quantify novel and established Tc radiopharmaceuticals. This method allows for fast on-site quality control of commercially available tracers and the characterization of novel experimental tracers in nuclear medicine without the need for cold reference compounds.
JOURNAL OF ANALYTICAL ATOMIC SPECTROMETRY
(2023)
Article
Chemistry, Analytical
Maximilian Horstmann, Melanie Austrup, Felix Busch, Andreas Faust, Michael Sperling, Uwe Karst, David Clases
Summary: This study presents a speciation analysis method using liquid chromatography and mass spectrometry to identify, characterize, and quantify Tc radiopharmaceuticals. The method allows fast on-site quality control and promotes the development of novel tracers in nuclear medicine.
JOURNAL OF ANALYTICAL ATOMIC SPECTROMETRY
(2023)
Review
Biochemistry & Molecular Biology
Alessandra Boschi, Licia Uccelli, Lorenza Marvelli, Corrado Cittanti, Melchiore Giganti, Petra Martini
Summary: Technetium-99m is the preferred radioisotope for myocardial perfusion tracers due to its favorable nuclear properties and rich coordination chemistry. However, the currently used tracers have various shortcomings. An ideal myocardial perfusion tracer should have high myocardial uptake, stable target-to-background ratio, low uptake in the lungs, liver, and stomach, high first-pass extraction fraction, rapid blood clearance, and linear relationship between myocardial uptake and coronary blood flow. Scientific research is focused on developing molecules that can meet these ideal characteristics as much as possible.
Article
Biochemistry & Molecular Biology
Antonio Shegani, Myrto Ischyropoulou, Ioanna Roupa, Christos Kiritsis, Konstantina Makrypidi, Afroditi Papasavva, Catherine Raptopoulou, Vassilis Psycharis, Heather M. Hennkens, Maria Pelecanou, Minas S. Papadopoulos, Ioannis Pirmettis
Summary: A series of 2 + 1 mixed ligand tricarbonyl complexes were synthesized, characterized, and evaluated, with diethyldithiocarbamate as a bidentate ligand and various monodentate ligands. The impact of the monodentate ligands on the synthesis and biodistribution of the complexes was significant.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Polymer Science
Nikolay Ivanovich Gorshkov, Andrei Yur'evich Murko, Yulia Igorevna Zolotova, Olga Vladimirovna Nazarova, Valerii Dmitrievich Krasikov, Sergei Vasilievich Shatik, Evgenii Fedorovich Panarin
Summary: The study investigated the preparation and characterization of N-vinylpyrrolidone-co-allylamine copolymers containing iminodiacetic chelation units with organometallic species, as well as optimal conditions for labeling the copolymers with radioactive Tc-99m(CO)(3)(+) species. The radiochemical yields reached 97% and the radiolabeled polymers showed stability in blood serum for at least 3 hours, with high primary accumulation in blood and subsequent excretion via the urinary tract in vivo distribution experiments in intact animals.
Article
Biochemistry & Molecular Biology
Konstantina Makrypidi, Christos Kiritsis, Ioanna Roupa, Sotiria Triantopoulou, Antonio Shegani, Maria Paravatou-Petsotas, Aristeidis Chiotellis, Maria Pelecanou, Minas Papadopoulos, Ioannis Pirmettis
Summary: This study synthesized a novel epidermal growth factor receptor tyrosine kinase inhibitor and successfully labeled it with a molybdenum complex using a ligand exchange reaction. The results showed that the labeled complex exhibited potential inhibitory effects on cancer cell growth.
Article
Chemistry, Multidisciplinary
Qaisar Nadeem, Federica Battistin, Olivier Blacque, Roger Alberto
Summary: A new method for the synthesis of sandwich type complexes from functionalized arenes and pharmaceuticals has been reported. The use of N-methylpyrrolidine facilitates the substitution of naphthalene with incoming arenes. The series of fully characterized rhenium sandwich complexes includes compounds formed with simple arenes and active compounds.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Chemistry, Multidisciplinary
Qaisar Nadeem, Federica Battistin, Olivier Blacque, Roger Alberto
Summary: A new synthesis method for sandwich type complexes, including functionalized arenes and pharmaceuticals, paves the way for molecular theranostics.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Chemistry, Inorganic & Nuclear
Saul M. Cooper, Andrew J. P. White, Thomas R. Eykyn, Michelle T. Ma, Philip W. Miller, Nicholas J. Long
Summary: N-Triphos derivatives are a class of tuneable, tripodal ligands that are related to the coordination chemistry of Re and Tc in biomedical applications. Mixed-ligand approaches can be used to obtain Tc complexes with different core structures and properties. It has been found that the properties of the ligands can affect the configuration and stability of the products.
INORGANIC CHEMISTRY
(2022)
Article
Medicine, Research & Experimental
Shahnaz Saednia, Saeed Emami, Sajjad Molavipordanjani, Seyed Mohammad Abedi, Fereshteh Talebpour Amiri, Seyed Jalal Hosseinimehr
Summary: This study aimed to develop novel tracers for targeting and imaging overexpressed serotonin-7 receptors in U-87 MG glioma xenografted nude mice. The radiotracers Tc-99m-PHH and Tc-99m-MPHH showed promising affinity and uptake in the tumor tissue, with Tc-99m-MPHH demonstrating higher affinity to 5-HT7Rs.
MOLECULAR PHARMACEUTICS
(2021)
Article
Biochemistry & Molecular Biology
Yongkyoung Kweon, Ji-Yong Park, Young-Joo Kim, Yun-Sang Lee, Jae-Min Jeong
Summary: This study demonstrates the detection of endogenous hydrogen sulfide generated in hypoxic tissue using [Tc-99m]Tc-gluconate, a novel imaging agent that can be used both in vitro and in vivo.
Article
Biochemistry & Molecular Biology
Raunak Varshney, Puja P. Hazari, Anjani K. Tiwari, Rashi Mathur, Aruna Kaushik, Meenakshi Saklani, Sweta Singh, Ankur Kaul, Roger Stromberg, Anil K. Mishra
Summary: The study focused on enhancing neuronal survival and regeneration using a synthetic peptide analog of gamma 1 laminin. By designing and modifying a KDI derivative, the potency towards neurite growth was increased. The synthesized peptide showed improved binding with the desired receptor for neurite growth, potentially useful for neurodegenerative disorders.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Ingebjorg N. Hungnes, Fahad Al-Salemee, Peter J. Gawne, Thomas Eykyn, R. Andrew Atkinson, Samantha Y. A. Terry, Fiona Clarke, Philip J. Blower, Paul G. Pringle, Michelle T. Ma
Summary: This study demonstrates the feasibility of using the diphosphine compound BMA as a platform for preparing receptor-targeted Tc-99m-labelled radiotracers, which are simple and practical to use. Utilizing optimized kit-based protocols, the radiotracer exhibited high metabolic stability and targeted specificity, showing promising potential for clinical applications.
DALTON TRANSACTIONS
(2021)
Article
Biochemistry & Molecular Biology
Ariadni Zianna, Elena Geromichalou, George Geromichalos, Augusta-Maria Fiotaki, Antonios G. Hatzidimitriou, Stavros Kalogiannis, George Psomas
Summary: The synthesis of five neutral zinc(II) complexes of 3,5-dibromo-salicyladehyde with nitrogen-donor co-ligands resulted in compounds with selective in vitro antibacterial activity, radical scavenging abilities, H2O2 reduction capabilities, ability to intercalate with DNA, and reversible binding to proteins. Molecular docking studies supported the in vitro findings, suggesting a potential mechanism of action for these complexes.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Ayat-Allah Mamdouh, Ahmed B. M. Ibrahim, Nour El-Houda A. Reyad, Tarek R. Elsayed, Isabel Cordeiro Santos, Antonio Paulo, Refaat M. Mahfouz
Summary: This paper presents the synthesis and characterization of two cluster compounds and investigates their antibacterial activity and thermal decomposition mechanisms. The nickel compound exhibits higher inhibitory activity against gram-positive bacteria and phytopathogenic bacteria, while the cobalt compound shows higher antibacterial activity against Pseudomonas aeruginosa.
JOURNAL OF CLUSTER SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
E. Halevas, S. Matsia, A. Hatzidimitriou, E. Geromichalou, T. A. Papadopoulos, G. Katsipis, A. Pantazaki, G. Litsardakis, A. Salifoglou
Summary: Quercetin is a bioactive flavonoid with limited solubility and bioavailability, but a synthetic ternary compound Ce(III)-quercetin-(1,10-phenanthroline) has shown enhanced bioavailability and bioactivity. Physicochemical characterization revealed its properties and biological studies demonstrated its toxicity-suppressing potential and cell metabolism inhibition. In silico studies provided insight into its mechanism of action at the molecular level. This work highlights the importance of metal-flavonoid compounds in enhancing the role of flavonoids in physiology and disease.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Eleftherios Halevas, Barbara Mavroidi, Georgia Zahariou, Maria Pelecanou, Antonios G. Hatzidimitriou
Summary: This article presents the advantages of using naringenin to chelate with metal ions and generate novel metal-based drugs, as well as the thorough characterization and antioxidant evaluation of two newly synthesized heteroleptic complexes of Cu(II) ion with naringenin and ancillary aromatic chelators.
INORGANICA CHIMICA ACTA
(2023)
Article
Biochemistry & Molecular Biology
Zisis Papadopoulos, Efstratia Doulopoulou, Ariadni Zianna, Antonios G. Hatzidimitriou, George Psomas
Summary: This article presents the synthesis, characterization, and biological profile of five neutral copper(II) complexes of 5-fluoro-salicylaldehyde in the absence or presence of N,N'-donor co-ligands. The compounds were characterized using physicochemical and spectroscopic techniques, and the crystal structures of four complexes were determined by single-crystal X-ray crystallography. The antioxidant capacity, interaction with calf-thymus DNA, and binding affinity with serum albumins were investigated.
Article
Pharmacology & Pharmacy
Andre Miranda, Roi Lopez-Blanco, Jessica Lopes-Nunes, Ana M. Melo, Maria Paula Cabral Campello, Antonio Paulo, Maria Cristina Oliveira, Jean-Louis Mergny, Paula A. Oliveira, Eduardo Fernandez-Megia, Carla Cruz
Summary: In this study, an aptadendrimer was synthesized by covalent bioconjugation of a gallic acid-triethylene glycol dendrimer with the G-quadruplex AT11 aptamer. The interaction between the aptadendrimer and the anticancer drug acridine orange ligand C-8 was evaluated. The aptadendrimer exhibited a diameter of approximately 3.1 nm. Both steady-state and time-resolved fluorescence anisotropy confirmed the interaction between the aptadendrimer and C-8. Release experiments demonstrated the delivery of C-8 after 4 h. Confocal microscopy revealed that the aptadendrimers localized in the cytoplasm of various cell lines. MTT studies showed high cytotoxicity mainly attributed to the C-8 ligand. These findings suggest that aptadendrimers have potential as nanocarriers.
Article
Biochemistry & Molecular Biology
Renan C. F. Leitao, Francisco Silva, Gabriel H. Ribeiro, Isabel C. Santos, Joana F. Guerreiro, Filipa Mendes, Alzir A. Batista, Fernando R. Pavan, Pedro Ivo da S. Maia, Antonio Paulo, Victor M. Deflon
Summary: Gallium and indium octahedral complexes with isoniazid derivative ligands were successfully synthesized. The complexes showed moderate affinity with human serum albumin through hydrophobic interactions. The complexes with H2L2 exhibited higher cytotoxicity against MCF-7 cells, as well as stronger accumulation in MCF-7 and PC-3 cells compared to the non-halogenated complexes. The ligands and metal complexes also demonstrated potent growth inhibitory effects against Mycobacterium tuberculosis.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2023)
Article
Chemistry, Medicinal
David Moreira, Jessica Lopes-Nunes, Fatima Milhano Santos, Maria Paula Cabral Campello, Maria Cristina Oliveira, Antonio Paulo, Candida Tomaz, Carla Cruz
Summary: AT11-L0 aptamer, which can adopt a G-quadruplex (G4) structure and target nucleolin (NCL), was characterized. The aptamer-functionalized liposomes were found to be stable and efficiently target NCL. However, AT11-L0 did not show anti-angiogenic effects.
Article
Chemistry, Inorganic & Nuclear
Leonor Corte-Real, Vivien Posa, Matilde Martins, Raquel Colucas, Nora V. May, Xavier Fontrodona, Isabel Romero, Filipa Mendes, Catarina Pinto Reis, Maria Manuela Gaspar, Joao Costa Pessoa, Eva A. Enyedy, Isabel Correia
Summary: In this study, three novel Schiffbases (L1-L3) derived from the condensation of 2-carbaldehyde-8-hydroxyquinoline with amines containing morpholine or piperidine moieties were synthesized and characterized. These Schiffbases were reacted with CuCl2 and ZnCl(2) to yield six new coordination compounds, which were all characterized using various techniques. The Cu(II) complexes showed higher stability and anticancer activity than the Zn(II) complexes.
INORGANIC CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Diogo M. M. Engracia, Catarina I. G. Pinto, Filipa Mendes
Summary: The application of cellular and animal models in drug development is limited due to translational significance, animal ethics, and inter-species physiological differences. 3D cellular models provide a more accurate representation of tissue complexity and reduce the use of animal models in biomedical research. In cancer research, 3D models can replicate the tumor microenvironment and help study anti-tumoral drugs with high selectivity and minimal toxicity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Julie Bolcaen, Mohamed A. Gizawy, Samantha Y. A. Terry, Antonio Paulo, Bart Cornelissen, Aruna Korde, Jonathan Engle, Valery Radchenko, Roger W. Howell
Summary: Auger electron (AE) radiopharmaceutical therapy (RPT) may have therapeutic efficacy similar to α-particles for small oncologic diseases, with lower risks of normal tissue toxicity. Despite accumulating knowledge about AE research, the promise of AE RPT has not yet been realized, with only a few agents evaluated in clinical trials.
JOURNAL OF NUCLEAR MEDICINE
(2023)
Article
Chemistry, Inorganic & Nuclear
Federica Battistin, Celia Fernandes, Paula. D. Raposinho, Olivier Blacque, Antonio Paulo, Roger Alberto
Summary: The pursuit of molecular imaging for tumors has led to the development of targeted approaches for epidermal growth factor receptors (EGFR). Recently, various Tc-99m-labeled EGFR inhibitors using quinazoline structures have been reported. Additionally, the integration of topoisomerase and tyrosine kinase inhibitors into Re and Tc-99m complexes has shown potential for tumor imaging.
DALTON TRANSACTIONS
(2023)
Article
Chemistry, Inorganic & Nuclear
Ariadni Zianna, Ellie Vradi, Antonios G. Hatzidimitriou, Stavros Kalogiannis, George Psomas
Summary: Five neutral zinc(ii) complexes were synthesized and characterized, and the crystal structures of complexes 1 and 3 were determined by single-crystal X-ray crystallography. These compounds exhibit DNA intercalation, moderate DNA cleavage, reversible binding to serum albumins, and antioxidant and antimicrobial activities.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Chrisoula Kakoulidou, Christos T. Chasapis, Antonios G. Hatzidimitriou, Konstantina C. Fylaktakidou, George Psomas
Summary: Two novel halogenated quinazoline derivatives were synthesized and characterized. The compounds showed interaction with metal(II) ions and exhibited various biological activities, including DNA interaction, cleavage ability, affinity to proteins, and antioxidant properties.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Inorganic & Nuclear
Despoina Varna, Elena Geromichalou, Antonios G. Hatzidimitriou, Rigini Papi, George Psomas, Panagiotis Dalezis, Paraskevas Aslanidis, Theodora Choli-Papadopoulou, Dimitrios T. Trafalis, Panagiotis A. Angaridis
Summary: In recent years, there has been increasing interest in studying Ag(I) coordination compounds as effective antibacterial and anticancer agents. This study synthesized a series of Ag(I) complexes with phosphines and heterocyclic thioamide ligands, and evaluated their antibacterial and anticancer properties. The results showed that some of these complexes exhibited potent activity against bacteria and cancer cells, with certain selectivity towards normal cells.
DALTON TRANSACTIONS
(2022)
Article
Biochemistry & Molecular Biology
Michael Ramek, Jasmina Sabolovic
Summary: This paper investigates the geometries, energy landscapes, and magnetic parameters of copper(II) amino acid compounds using density functional theory calculations. The results show that certain conformers with histaminate-like and glycine-like modes have low Gibbs free energies and high metal-binding affinities. The predicted conformations reproduce the experimental electron paramagnetic resonance parameters.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Wei Tian, Wen Zhong, Zengyan Yang, Ling Chen, Shijie Lin, Yanping Li, Yuxing Wang, Peilin Yang, Xing Long
Summary: A series of novel dibutyltin complexes based on salen-like ligands were synthesized and characterized. Complex S03 showed excellent in vitro anticancer activity and induced cancer cell death through multiple mechanisms. This study reveals new mechanisms of organotin complexes and provides new insights into the development of organotin metal complexes as anticancer drugs.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Natalie C. Korkola, Martin J. Stillman
Summary: Many proteins require a metal cofactor for their function, and these metals play a role in protein folding. The study found that the metallation rates of different metal binding pathways are influenced by pH, with the less cooperative pathway being more affected by low pH conditions. Specific mixtures of structures are formed in the initial steps of metallation, and unfolding the disordered apo-MT structure hinders the formation of these preliminary structures. The compact conformation of the native apo-MT allows for rapid formation of metal-thiolate structures with high affinity, providing protection from oxidation.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Boxuan Yang, Xitong Song, Binju Wang
Summary: The diiron active site plays a crucial role in catalytic transformations in both biological and chemical systems. Recent advancements in the field include the synthesis of biomimetic diiron catalysts inspired by the active structure of soluble methane monooxygenase (sMMO), which have been successfully applied to the dehydrogenation of indolines.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2024)
Article
Biochemistry & Molecular Biology
Christina N. Banti, Angeliki A. Piperoudi, Catherine P. Raptopoulou, Vassilis Psycharis, Constantinos M. Athanassopoulos, Sotiris K. Hadjikakou
Summary: Two copper(I) polymorphs with mitochondria-targeting properties were successfully prepared via metal ion conjugation. These compounds showed promising activities in DNA binding, enzyme inhibition, and cancer cell inhibition. The molecular mechanisms of action were investigated.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2024)