Article
Chemistry, Organic
Zijun Chen, Gianluca Destro, Florian Guibbal, Chung Ying Chan, Bart Cornelissen, Veronique Gouverneur
Summary: This study presents two strategies for accessing the F-18-isotopologue of rucaparib using a copper-mediated nucleophilic F-18-fluorodeboronation. The most successful approach involves an aldehydic boronic ester precursor and reductive amination post-F-18-labeling, resulting in [F-18]rucaparib with a high activity yield and molar activity. Preliminary in vitro studies showed promising results.
Article
Chemistry, Medicinal
Valentina Di Iorio, Stefano Boschi, Anna Sarnelli, Cristina Cuni, David Bianchini, Manuela Monti, Giancarlo Gorgoni, Giovanni Paganelli, Federica Matteucci, Carla Masini
Summary: This study verified the feasibility of using [F-18]F- from different external suppliers to produce [F-18]F-PSMA-1007. The results showed no significant differences in terms of radionuclidic and radiochemical purity between the two suppliers, and the quality control parameters were unaffected.
Article
Chemistry, Multidisciplinary
Jay S. Wright, Richard Ma, E. William Webb, Wade P. Winton, Jenelle Stauff, Kevin Cheng, Allen F. Brooks, Melanie S. Sanford, Peter J. H. Scott
Summary: This report presents the development of a Zn(OTf)(2)-mediated method for converting alpha-tertiary haloamides to the corresponding alpha-tertiary fluoroamides. Under optimized conditions, high radiochemical conversion can be achieved. This method has been successfully applied to prepare various model radiofluorides.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Organic
Dong Zhou, John A. Katzenellenbogen
Summary: A simple continuous-flow solid-phase radiosynthesis method has been developed for the direct generation of [F-18] triflyl fluoride from [F-18] fluoride, allowing for the preparation of F-18 labeled radiopharmaceuticals with high efficiency and safety.
TETRAHEDRON LETTERS
(2021)
Review
Chemistry, Multidisciplinary
Mitchell A. Klenner, Giancarlo Pascali, Massimiliano Massi, Benjamin H. Fraser
Summary: PET-fluorescence imaging is an emerging field that combines positron emission tomography and fluorescence imaging techniques, utilizing probes containing fluorophores and radioisotopes to provide complementary information. Different fluorine-18 labelled PET-fluorescence probes have been classified into four groups based on the implemented fluorophore, with a systematic comparison of their properties to aid future endeavors in PET-fluorescence chemistry.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Article
Chemistry, Analytical
Kuang Chen, Xiaojun Zhang, Fei Wang, Yitian Wu, Haoxi Zhou, Ying Zhang, Wenbo Zou, Jinming Zhang, Rong Liu
Summary: This study evaluated the potential of [F-18]AlF-RESCA-ICG in assessing hepatic function reserve on PET/CT imaging. The results showed that this labeled agent can accurately assess liver function and is of great significance for diagnosing liver diseases.
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY
(2022)
Article
Neurosciences
Yanxiao Li, Yee Ling Ng, Manish D. Paranjpe, Qi Ge, Fengyun Gu, Panlong Li, Shaozhen Yan, Jie Lu, Xiuying Wang, Yun Zhou
Summary: This study aimed to improve the statistical power in detecting changes in brain glucose metabolism, amyloid, and tau deposition in Alzheimer's disease studies by using a reference tissue-based quantification approach. The results showed that the tracer-specific reference tissue improved the detection of PET SUVR changes, which is beneficial for early diagnosis, disease progression monitoring, and therapeutic response in Alzheimer's disease.
HUMAN BRAIN MAPPING
(2022)
Article
Chemistry, Organic
Lin Qiu, Hao Jiang, Yanbo Yu, Jiwei Gu, Jinzhi Wang, Haiyang Zhao, Tianyu Huang, Robert J. Gropler, Robyn S. Klein, Joel S. Perlmutter, Zhude Tu
Summary: The study has developed a new multiple step F-18 labeling strategy, successfully synthesized the [F-18]FS1P1 radiotracer with the same structure as the existing tracer [C-11]CS1P1. The radiotracer showed high metabolic stability and effective method for detecting neuroinflammatory status in animal models.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Kazunori Kawamura, Katsushi Kumata, Wakana Mori, Masayuki Fujinaga, Yusuke Kurihara, Masanao Ogawa, Takayuki Ohkubo, Kenji Furutsuka, Hiroki Hashimoto, Nobuki Nengaki, Ming-Rong Zhang
Summary: A method for F-18-fluoroethylation without azeotmpic drying of cyclotron-produced [F-18]F- has been developed, enabling simplified automated radiosynthesis of [F-18]fluoroethylated tracers, [F-18]FEDAC and [F-18]FET, with radiochemical yields of 26 +/- 3.7% and 14 +/- 2.2% respectively.
APPLIED RADIATION AND ISOTOPES
(2021)
Review
Oncology
Domenico Albano, Giorgio Treglia, Francesco Dondi, Anna Calabro, Alessio Rizzo, Salvatore Annunziata, Luca Guerra, Silvia Morbelli, Alessandra Tucci, Francesco Bertagna
Summary: The new biomarker Dmax, which measures the maximal distance between the two farthest hypermetabolic PET lesions, has shown high accuracy as a prognostic factor in lymphoma patients. Most studies have demonstrated the significant predictive value of Dmax in predicting progression-free survival and overall survival.
Article
Engineering, Environmental
Zheng Fu, Lun Yu, Yongkang Gai, Feng Gao, Quanyi Liu, Li Wang, Zhiguo Liu
Summary: The construction of a fully automated Al[18F]F radiochemistry system can improve the reproducibility and reliability of Al[18F]F-based radiopharmaceuticals, and facilitate the translation from preclinical to clinical studies. This study aimed to address the limitations of commercially available automated radiosynthesizers by designing, assembling, and validating a custom-built radiosynthesizer for the production of clinical-grade Al[18F]F tracers.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Multidisciplinary Sciences
Pardeep Kumar, Riptee Thakur, Pratap Chandra Acharya, Hosahalli K. Mohan, U. N. Pallavi, Divya Maheshwari, Afsal K. M. Mohammed, Aishwarya Kumar, Sridhar Goud Nerella, Raman Kumar Joshi, Manoj Kumar, Chandana Nagaraj
Summary: The study successfully synthesized a F-18 labeled tracer AVT-011 and demonstrated its specificity for Pgp and safety for patient use.
SCIENTIFIC REPORTS
(2022)
Article
Chemistry, Medicinal
Verena Hugenberg, Marion Zerna, Mathias Berndt, Reinhard Zabel, Rainer Preuss, Dirk Rolfsmeier, Janet Wegener, Henrik Fox, Astrid Kassner, Hendrik Milting, Norman Koglin, Andrew W. Stephens, Jan F. Gummert, Wolfgang Burchert, Marcus-Andre Deutsch
Summary: This study presents a novel radiotracer [F-18]GP1 for clinical applications in the cardiovascular field. With improved synthesis methods and validation processes to GMP standards, [F-18]GP1 has been successfully implemented for visualization of active platelet aggregation at the molecular level, providing a highly sensitive tool for clinical use.
Article
Radiology, Nuclear Medicine & Medical Imaging
Abarnaa Sivapathasundaram, Nicolas Golse, Alina Pascale, Emmanuel Durand, Mylene Sebagh, Florent L. Besson
Summary: Contrary to common belief, F-18-FDG/F-18-choline dual-tracer PET behavior is not a relevant surrogate of tumor differentiation in hepatocellular carcinoma (HCC). Future multitracer PET studies are necessary to improve our understanding of their biological significance in this field.
CLINICAL NUCLEAR MEDICINE
(2023)
Article
Biochemical Research Methods
Yingqing Lu, Yingfang He, Roger Schibli, Linjing Mu, R. Michael van Dam
Summary: Copper-mediated radiofluorination has great potential in the synthesis of PET radioligands. We demonstrated the feasibility of Cu-mediated radiosynthesis on a high-throughput microdroplet platform and optimized the reaction conditions. By utilizing microscale conditions, we achieved higher radiochemical yield and excellent radiochemical purity and molar activity. We also successfully translated these optimized conditions to a vial-based method, expanding the applicability of the synthesis approach.
Article
Chemistry, Medicinal
Federico Luzi, Vilius Savickas, Carlotta Taddei, Stefan Hader, Nisha Singh, Antony D. Gee, Salvatore Bongarzone
FUTURE MEDICINAL CHEMISTRY
(2020)
Article
Chemistry, Physical
Andreas Mavroskoufis, Michael Jakob, Matthew N. Hopkinson
Article
Chemistry, Organic
Matthew N. Hopkinson, Andreas Mavroskoufis
Summary: Excitation of carbonyl groups is a widely used activation mode in photochemistry, but many transformations are limited to aldehydes and ketones. This study introduces a novel strategy using N-heterocyclic carbene (NHC) organocatalyst to enable "ketone-like" photochemistry with carboxylic acid derivatives, demonstrating the feasibility of photoenolization/Diels-Alder reactions.
Article
Chemistry, Organic
Armin Ariamajd, Nils J. Gerwien, Benjamin Schwabe, Stefan Dix, Matthew N. Hopkinson
Summary: A series of BT-SRF salts have been synthesized for the first time, providing a convenient source of perfluoroalkylthiolate anions. These salts were found to react in a deoxygenative nucleophilic substitution reaction, leading to the direct synthesis of pentafluoroethyl and heptafluoropropyl thioethers from readily available alcohols.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Biochemical Research Methods
Francesca Goudou, Antony D. Gee, Salvatore Bongarzone
Summary: A copper-catalysed radiosynthesis was developed to obtain carbon-11-labelled carboxylic acids by reacting terminal alkynes with cyclotron-produced carbon-11 carbon dioxide in the presence of DBU. This method resulted in a small library of C-11-labelled propiolic acid derivatives with radiochemical yields ranging from 7% to 28% in a total synthesis time of 15 min from end of bombardment (EOB).
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
(2021)
Article
Chemistry, Multidisciplinary
Stefan Dix, Paul Golz, Jonas R. Schmid, Sebastian Riedel, Matthew N. Hopkinson
Summary: The introduction of bis(trifluoromethyl)peroxide as a practical trifluoromethoxylating reagent opens up a new and efficient method for preparing trifluoromethoxylated arenes. This reagent, easily accessible from inexpensive bulk chemicals, allows for the preparation of trifluoromethoxylated arenes in good yields under mild conditions directly from unactivated aromatics using visible light photoredox or TEMPO catalysis. Additionally, TEMPO catalysis enables the one-step synthesis of valuable pyridine derivatives, simplifying the synthetic process.
CHEMISTRY-A EUROPEAN JOURNAL
(2021)
Review
Chemistry, Multidisciplinary
Peter Bellotti, Maximilian Koy, Matthew N. Hopkinson, Frank Glorius
Summary: N-Heterocyclic carbenes have attracted significant interest due to their versatility, modularity and strong coordinating properties, leading to a rapid increase in utilization across various fields in the past decade. Future directions and recent developments in the field are also highlighted in this review.
NATURE REVIEWS CHEMISTRY
(2021)
Article
Chemistry, Organic
Andreas Mavroskoufis, Arielle Rieck, Matthew N. Hopkinson
Summary: The photochemical reactivity of acyl azolium salts derived from aliphatic carboxylic acids was investigated, showing Norris type II elimination reactions and Norris-Yang cyclization under UVA light irradiation. These results demonstrate the influence of NHCs on the absorption properties and photochemical reactivity of carbonyl groups during a catalytic cycle.
Review
Chemistry, Multidisciplinary
Antonio Shegani, Steven Kealey, Federico Luzi, Filippo Basagni, Joana do Mar Machado, Sevban Dogan Ekici, Alessandra Ferocino, Antony D. Gee, Salvatore Bongarzone
Summary: The presence of PET centers at major hospitals and the improvement of PET scanner sensitivity have increased interest in PET tracer development using carbon-11. Methodological improvements and automated modules have allowed the development of carbon-11 tracers for clinical use. Radiolabeling natural compounds with carbon-11 has provided important information on their biochemistry and in vivo behavior.
Article
Chemistry, Medicinal
Igor C. Fontana, Debora G. Souza, Diogo O. Souza, Antony Gee, Eduardo R. Zimmer, Salvatore Bongarzone
Summary: The excitatory amino acid transporter 2 (EAAT2) is crucial for the clearance and recycling of glutamate, the major excitatory neurotransmitter in the brain. Dysfunctions in EAAT2 can lead to neurodegenerative diseases, such as ALS and AD. Detecting EAAT2 in the living human brain is important for improving diagnosis and therapy for these diseases. This article discusses the role of EAAT2 and presents potential activators for therapy and molecular imaging tools for diagnosis.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Correction
Chemistry, Medicinal
Igor C. Fontana, Debora G. Souza, Diogo O. Souza, Antony Gee, Eduardo R. Zimmer, Salvatore Bongarzone
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Correction
Chemistry, Multidisciplinary
Antonio Shegani, Steven Kealey, Federico Luzi, Filippo Basagni, Joana do Mar Machado, Sevban Dogan Ekici, Alessandra Ferocino, Antony D. Gee, Salvatore Bongarzone
Article
Chemistry, Multidisciplinary
Tatsuya Kikuchi, Masanao Ogawa, Toshimitsu Okamura, Antony D. Gee, Ming-Rong Zhang
Summary: This study reports a simple and efficient method for the production of [C-11]HCN that can be easily implemented in C-11 production facilities, eliminating the need for a dedicated infrastructure.
Review
Chemistry, Organic
Federico Luzi, Antony D. Gee, Salvatore Bongarzone
Summary: PET requires positron-emitting nuclides, with C-11 being advantageous due to the ubiquity of carbon atoms in biomolecules, but quick, robust, and chemospecific radiolabelling strategies are needed due to its short half-life and low production scale. The use of silicon-based chemistry for C-11-labelling has been proposed as a rapid and effective method, showing broad applicability and high efficiency in organic chemistry.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Julia E. Blower, Michelle T. Ma, Fahad A. I. Al-Salemee, Antony D. Gee
Summary: Nitrogen-13 is a PET radionuclide that can be used to label molecules of biological and pharmaceutical interest despite its short half-life. By adapting a specific synthetic reaction, a library of labeled compounds can be prepared, which has significant implications for clinical applications.
CHEMICAL COMMUNICATIONS
(2021)
Article
Chemistry, Multidisciplinary
Alexander M. Prophet, Kritanjan Polley, Gary J. Van Berkel, David T. Limmer, Kevin R. Wilson
Summary: The oxidation kinetics of iodide by ozone at the air-water interface is studied in single microdroplets. Molecular simulations and kinetic modeling are used to understand the underlying multiphase mechanism.
Article
Chemistry, Multidisciplinary
Rong Zhang, Jiajing Lan, Fei Wang, Shumei Chen, Jian Zhang
Summary: By utilizing 1,1'-ferrocene dicarboxylic acid as a chelating and surface protection ligand, we have synthesized multi-nuclear indium oxide clusters with varying nuclear sizes, including heptanuclear and thirteen-nuclear clusters. These clusters possess labile coordination sites, allowing for structural modification and self-assembly, resulting in the formation of various cluster structures.
Article
Chemistry, Multidisciplinary
Hui Wang, Hui Liu, Mingsen Wang, Jiaheng Hou, Yongjun Li, Yuancheng Wang, Yingjie Zhao
Summary: Two supramolecular complexes were prepared using CBs and M1, and their single-crystal structures were analyzed by SCXRD. The unexpected 1:2 self-assembly structure between M1 and CB[8] was discovered for the first time. These complexes exhibit unique photophysical properties and provide valuable information about the structure and photophysical properties of supramolecular complexes.
Article
Chemistry, Multidisciplinary
Chang-Hee Lee, Sookil Park, Sanggil Kim, Ji Young Hyun, Hyun Soo Lee, Injae Shin
Summary: The epidermal growth factor receptor (EGFR) is a cell-surface glycoprotein involved in cell proliferation and tumor development. This study used a fluorescently labeled EGFR to investigate its time-dependent endocytosis in live cells and found that appended glycans affect EGFR internalization. Additionally, the study detected sialic acid residues attached to EGFR on the live cell surface using FRET-based imaging. This research provides valuable insights into the cellular functions of EGFR.
Article
Chemistry, Multidisciplinary
Subhankar Sahu, Lokesh Kumar, Sumita Das, Dipti Gupta, Ruchi Anand
Summary: This study proposes a strategy that combines organic electronics with biosensor scaffolds to create a compact device for monitoring environmental aromatic pollution. By coupling biosensing protein MopR with an organic electrochemical transistor (OECT), a sensor module capable of efficient detection of phenol was designed. Exclusive phenol detection with minimal loss of sensitivity could be achieved in complex pollutant mixtures and real environmental samples.
Review
Chemistry, Multidisciplinary
Changseok Lee, Hyung-Joon Kang, Sungwoo Hong
Summary: The formation of C-N bonds through hydroamination reactions catalyzed by nickel hydrides has been a topic of recent interest. This approach offers a way to efficiently transform a variety of alkene and alkyne substrates into compounds enriched with C-N bonds. The review provides a concise overview of the underlying reaction mechanisms and aims to stimulate further progress in NiH-catalytic techniques and catalyst design.
Article
Chemistry, Multidisciplinary
Yueci Wu, Lu-Lu Sun, Hai-Hao Han, Xiao-Peng He, Weiguo Cao, Tony D. James
Summary: Drug-induced liver injury (DILI) is a common cause of acute liver failure in the USA and Europe, but most cases can be recovered or prevented by discontinuing the offending drug. Recent research has found that peroxynitrite (ONOO-) can be used as a potential indicator for early diagnosis of DILI, and there is an urgent need to establish a method to detect and track peroxynitrite in DILI cases. In this study, a FRET-based nano fluorescent probe CD-N-I was developed, which showed high selectivity and sensitivity in detecting peroxynitrite. The probe successfully detected exogenous peroxynitrite in live cells and endogenous peroxynitrite in APAP-induced liver injury of HepG2 cells.
Article
Chemistry, Multidisciplinary
Dmitry L. Lipilin, Mikhail O. Zubkov, Mikhail D. Kosobokov, Alexander D. Dilman
Summary: This article describes a direct photocatalytic method for the thiolation of unprotected acids, which was previously challenging. By using a thionocarbonate reagent with an N-O bond, the efficient conversion of carboxylic acids to thiols is achieved.
Article
Chemistry, Multidisciplinary
Jason Malenfant, Lucille Kuster, Yohann Gagne, Kouassi Signo, Maxime Denis, Sylvain Canesi, Mathieu Frenette
Summary: Raman microscopy can reveal compound-specific vibrational fingerprints without sample preparation. The combination of efficient theoretical calculations and a user-friendly software can accurately predict peak positions and provide match scores to assist with structure determination.
Article
Chemistry, Multidisciplinary
Jayoh A. Hernandez, Paul S. Micus, Sean Alec Lois Sunga, Luca Mazzei, Stefano Ciurli, Gabriele Meloni
Summary: Essential trace metals play crucial roles in the survival and virulence of bacterial pathogens. Helicobacter pylori requires nickel for colonization and persistence in the stomach, and NixA is an essential nickel transporter in this process. This study characterizes the selectivity and electrogenic nature of NixA-mediated nickel transport.
Article
Chemistry, Multidisciplinary
Tarali Devi, Kuheli Dutta, Jennifer Deutscher, Stefan Mebs, Uwe Kuhlmann, Michael Haumann, Beatrice Cula, Holger Dau, Peter Hildebrandt, Kallol Ray
Summary: This study emphasizes the importance of subtle electronic changes and secondary interactions in the stability of biologically relevant metal-dioxygen intermediates. It also shows that the role of the chloride ligand in stabilizing the Fe-III-(OOBu)-Bu-t moiety can extend to other anions, including the thiolate ligand.
Article
Chemistry, Multidisciplinary
Jacqueline R. Santhouse, Jeremy M. G. Leung, Lillian T. Chong, W. Seth Horne
Summary: By studying the folding kinetics and mechanism of the BdpA sequence, researchers found that altering the backbone connectivity can affect protein folding. This suggests that protein mimetic chains have a significant degree of plasticity in transitioning between unfolded and folded states.
Article
Chemistry, Multidisciplinary
Divanshu Gupta, Ralf Einholz, Holger F. Bettinger
Summary: This study presents the first direct spectroscopic evidence of a cyclic seven-membered iminoborane. Compared to linear amino-iminoboranes, this cyclic iminoborane exhibits weakened bond strength and lower Lewis acidity value. The study suggests that the reduced ring strain of cyclic iminoborane prevents nitrogen fixation but allows facile (2 + 2) cycloaddition reaction with C2H4.
Article
Chemistry, Multidisciplinary
Renny Mathew, Aniruddha Mazumder, Praveen Kumar, Julie Matula, Sharmarke Mohamed, Petr Brazda, Mahesh Hariharan, Brijith Thomas
Summary: This study reveals the packing arrangement of partially disordered nitro-perylenediimide (NO2-PDI) using a synergistic approach that combines 3D ED, ssNMR, and DFT techniques. By overcoming these challenges, this methodology opens up new avenues for material characterization, driving exciting advancements in the field.
