Article
Chemistry, Physical
Tao Tong, Mark Douthwaite, Lu Chen, Rebecca Engel, Matthew B. Conway, Wanjun Guo, Xin-Ping Wu, Xue-Qing Gong, Yanqin Wang, David J. Morgan, Thomas Davies, Christopher J. Kiely, Liwei Chen, Xi Liu, Graham J. Hutchings
Summary: The physicochemical properties of Pt/CeO2 catalysts were varied to investigate their impact on the hydrogen-borrowing amination of alcohols. It was found that the Pt precursor and CeO2 support properties strongly influenced catalytic performance. The most active catalyst exhibited linearly structured Pt species, which were more effective for the rate-determining step of cyclopentanol dehydrogenation compared to Pt clusters and nanoparticles. This study not only provides insights into desirable catalytic properties for hydrogen-borrowing amination but also has broader relevance to related fields.
Article
Chemistry, Organic
Yang Li, Arshad Ali, Junchao Dong, Yu Zhang, Lili Shi, Qun Liu, Junkai Fu
Summary: Using a directing-group strategy, a copper-catalyzed diamination of unactivated alkenes efficiently generates symmetrical diamines with high diastereoselectivity using readily available dialkylamines as amino sources, while unsymmetrical diamines require a one-pot or two-step operation. These reactions are proposed to proceed through aziridinium intermediates.
Article
Chemistry, Multidisciplinary
Rok Narobe, Kathiravan Murugesan, Christoph Haag, Tobias Emanuel Schirmer, Burkhard Koenig
Summary: Visible light excitation of iodine(iii)-BF3 complex enables the formation of carbocations from C(sp(3))-H bonds. The complexes are generated catalytically from iodoarene, carboxylate ligand, the oxidizing agent Selectfluor, and the Lewis acid BF3. This modular catalytic system allows the formation of synthetically valuable amine derivatives without a metal- or photocatalyst.
CHEMICAL COMMUNICATIONS
(2022)
Article
Chemistry, Multidisciplinary
Qing Liu, Linhong Long, Pengchen Ma, Yingjie Ma, Xuebing Leng, Jie Xiao, Hui Chen, Liang Deng
Summary: An isolable iron(IV) imido complex with trifluoromethyl on nitrogen, [(IPr)Fe(NC(CF3)(2)Ph)(2)], was reported, demonstrating long Fe-N(imido) bonds, bent Fe-N(imido)-C(imido) alignments, and the ability to undergo intramolecular C-H bond activation reaction to transform into an iron(II) amido complex. Theoretical study suggests a hydrogen-atom-abstraction mechanism in the C-H bond activation reaction with low activation barrier due to the electron-withdrawing nature of the trifluoromethyl group.
CELL REPORTS PHYSICAL SCIENCE
(2021)
Article
Chemistry, Multidisciplinary
Qi Zhao, Lirong Zheng, Yixuan Gao, Jingjing Li, Juanjuan Wei, Min Zhang, Jianghui Sun, Jin Ouyang, Na Na
Summary: An aptamer-functionalized Pd@MoO3-x nano-hydrangea (A-Pd@MoO3-x NH) with dual active centers has been developed to overcome the adverse effects of the tumor microenvironment (TME) and achieve high-efficiency cancer therapy. This nanozyme can address tumor hypoxia and high endogenous glutathione (GSH) through cascade enzymatic reactions, catalyzing the degradation of GSH and mitigating the accumulation of cytotoxic superoxide radicals in TME.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Engineering, Electrical & Electronic
Keila Silva dos Santos, Gustavo Oliveira Cavalcanti, Antonio Azevedo, Crislane Priscila do Nascimento Silva, Marcos Tavares de Melo, Ignacio Llamas-Garro, Eduardo Fontana
Summary: This article presents the analysis, design, and construction of a microstrip device for hydrogen detection at microwave frequencies. The device consists of a hybrid microstrip line with a 10-nm-thick palladium film replacing part of the copper line. Experimental results and theoretical modeling indicate that the phase of the scattering parameter S-21 becomes highly sensitive to the conductivity of the palladium when a thin film is used, enabling effective hydrogen detection. This finding suggests the possibility of incorporating ultrathin palladium films into planar microwave circuits for the development of simple hydrogen sensors.
IEEE SENSORS JOURNAL
(2023)
Article
Chemistry, Multidisciplinary
Dong Wei, Han-Yu Lu, Han-Zhe Miao, Chen-Guo Feng, Guo-Qiang Lin, Yingbin Liu
Summary: An efficient and environmentally friendly method for preparing substituted indene derivatives using water as the sole solvent has been developed. This reaction can be conducted under air, tolerates a wide range of functional groups, and can be easily scaled up. Bioactive natural products like indriline can be synthesized using this protocol. Preliminary results show the possibility of achieving enantioselectivity.
Article
Chemistry, Multidisciplinary
Yi Yu, Xiao-Bin Zhu, Yaofeng Yuan, Ke-Yin Ye
Summary: The widespread use of tetrazoles in various fields has driven the development of efficient and selective synthesis methods. However, the synthesis of diverse tetrazoles using abundant and inexpensive chemical feedstocks such as alkanes and alkenes remains challenging. In this study, an electrochemical multicomponent reaction (e-MCR) was developed for the highly efficient and selective synthesis of C-H tetrazolation of alkyl arenes. Additionally, this method also enabled the synthesis of versatile vicinal azidotetrazoles, which have potential applications as building blocks and high-energy materials.
Article
Chemistry, Physical
Caitlin M. Crombie, Richard J. Lewis, David Kovacic, David J. Morgan, Thomas J. A. Slater, Thomas E. Davies, Jennifer. K. Edwards, Martin Skov Skjoth-Rasmussen, Graham J. Hutchings
Summary: The oxidation of cyclohexane via in-situ production of H2O2 offers an attractive route to producing cyclohexanone and cyclohexanol. The introduction of V into a supported Pd catalyst significantly improves KA oil concentration. This improvement is attributed to the development of Pd domains with mixed oxidation state upon V incorporation.
Article
Chemistry, Physical
Caitlin M. Crombie, Richard J. Lewis, David Kovacic, David J. Morgan, Thomas E. Davies, Jennifer. K. Edwards, Martin Skov Skjoth-Rasmussen, Graham J. Hutchings
Summary: This study demonstrates that the in-situ production of H(2)O(2) by AuPd nanoparticles can catalyze the oxidation of cyclohexane to form KA oil under conditions where activity is limited when using molecular O-2, with no loss in catalytic activity observed upon re-use. The effect of key reaction parameters, including reaction temperature, catalyst mass and H-2:O(2) ratio, are evaluated.
Article
Chemistry, Multidisciplinary
Luiz F. T. Novaes, Justin S. K. Ho, Kaining Mao, Kaida Liu, Mayank Tanwar, Matthew Neurock, Elisia Villemure, Jack A. Terrett, Song Lin
Summary: In this study, we developed a novel electrochemical method for the selective α-methylation of protected amines, which are structurally complex medicinal agents. This method demonstrates broad reaction scope, high functional group compatibility, and allows for late-stage functionalization of complex targets containing basic nitrogen groups. Additionally, this method can be combined with organozinc-mediated C-C bond formation, enabling the direct methylation of various amine derivatives and potentially accelerating drug discovery efforts.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Multidisciplinary
T. Parker Maloney, Alexander F. Dohoda, Alec C. Zhu, Forrest E. Michael
Summary: In this study, we reported a convenient and transition metal-free intermolecular propargylic C-H amination of alkynes. The reaction showed high yields for terminal, silyl, and internal alkynes with a wide range of functional groups. The regioselectivity of amination was found to be influenced by substitution pattern and relatively remote heteroatomic substituents.
Article
Chemistry, Organic
Zhoumei Tan, Fang Xiang, Kun Xu, Chengchu Zeng
Summary: This paper reports a new method for the hydroazolylation of alkenes with azoles under external oxidant-free conditions with low catalyst loadings.
Article
Chemistry, Physical
Caitlin M. Crombie, Richard J. Lewis, Rebekah L. Taylor, David J. Morgan, Thomas E. Davies, Andrea Folli, Damien M. Murphy, Jennifer K. Edwards, Jizhen Qi, Haoyu Jiang, Christopher J. Kiely, Xi Liu, Martin Skov Skjoth-Rasmussen, Graham J. Hutchings
Summary: The study demonstrates that bimetallic Pd-Fe catalysts supported on TiO2 are highly effective in oxidizing benzyl alcohol to benzaldehyde through the in situ production of H2O2. The enhanced activity of Pd-Fe catalysts, compared to other analogues, can be attributed to their bifunctionality for synthesizing H2O2 and catalyzing the production of oxygen-based radical species.
Article
Chemistry, Organic
Karli R. Holman, Allison M. Stanko, Matthieu J. R. Richter, Sean S. Feng, Mahideremariyam N. Gessesse, Sarah E. Reisman
Summary: In this study, radical and transition metal-catalyzed cascade cyclization strategies were explored for the synthesis of the tetracyclic core of the augustamine-type Amaryllidaceae alkaloids. The successful synthesis of noraugustamine and the development of an oxidative Heck/aza-Wacker cascade that forms multiple bonds and a quaternary carbon center in a single step were achieved.
Article
Biochemistry & Molecular Biology
Anna Tesei, Michela Cortesi, Martina Bedeschi, Noemi Marino, Giacomo Rossino, Roberta Listro, Daniela Rossi, Pasquale Linciano, Simona Collina
Summary: Different pathological conditions, including viral infections and cancer, can severely damage the cell by causing endoplasmic reticulum (ER) stress. In particular, coronavirus infections, such as COVID-19, result in ER stress due to the synthesis of large amounts of viral glycoproteins and disruption of ER homeostasis. ER stress plays a crucial role in the viral life cycle and tumor growth, metastasis, and response to therapies in cancer. Researchers have identified the antiplatelet agent ticlopidine as a potential intervention for ER stress induced by viral infections and cancer.
Article
Chemistry, Organic
Federico Casti, Rita Mocci, Andrea Porcheddu
Summary: Two easily accessible methods for preparing a variety of formylated and acetylated amines under mechanochemical conditions are presented. These two methodologies have complementary features, as they allow for the derivatization of aliphatic and aromatic amines.
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Roberta Listro, Alessio Malacrida, Francesca Alessandra Ambrosio, Giacomo Rossino, Marcello Di Giacomo, Valeria Cavalloro, Martina Garbagnoli, Pasquale Linciano, Daniela Rossi, Guido Cavaletti, Giosue Costa, Stefano Alcaro, Mariarosaria Miloso, Simona Collina
Summary: The research team isolated a secondary metabolite called Hib-ester from Hibiscus Sabdariffa L. calyces, which possesses antiproliferative properties against human MM. Compound 13 and 14 were found to be more potent than Hib-ester, providing a new chemical class for developing possible drug candidates.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Federico Cuccu, Francesco Basoccu, Claudia Fattuoni, Andrea Porcheddu
Summary: This article presents a mechanochemical acylation procedure based on acyl-saccharin derivatives, providing a valuable solvent-free alternative with rapid and user-friendly workup for multi-step procedures.
Article
Chemistry, Applied
Silvia Gaspa, Luca Ledda, David d'Atri, Andrea Porcheddu, Luisa Pisano, Massimo Carraro, Lidia De Luca
Summary: An esterification of the C-H bond of aldehydes is achieved using oxidovanadium(IV) sulfate as a catalyst. The reaction is facilitated by visible-light irradiation, performed at room temperature, and requires no additives, with H2O2 as the benign oxidant. This study showcases the potential of vanadium salts in halogenation processes, C-H activation, and contributes to the field of earth-abundant metal-based catalysis.
ADVANCED SYNTHESIS & CATALYSIS
(2023)
Article
Chemistry, Medicinal
Pasquale Linciano, Claudia Sorbi, Giacomo Rossino, Daniela Rossi, Andrea Marsala, Nunzio Denora, Martina Bedeschi, Noemi Marino, Giacomo Miserocchi, Giulio Dondio, Marco Peviani, Anna Tesei, Simona Collina, Silvia Franchini
Summary: In this study, novel benzylpiperidine/benzylpiperazine-based compounds were designed and tested as Sigma-1 receptor (S1R) agonists. The compounds 6b and 8b showed high affinity for S1R and selectivity over S2R and NMDAR. They exhibited neuroprotective activity and enhanced neurite outgrowth in cell lines, as well as good efficacy/safety profile in in-vitro and in-vivo models. These results encourage further preclinical investigations of compounds 6b and 8b on neurodegenerative diseases.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Claudia Sorbi, Silvia Belluti, Claudio Giacinto Atene, Federica Marocchi, Pasquale Linciano, Neena Roy, Elia Paradiso, Livio Casarini, Simone Ronsisvalle, Tommaso Zanocco-Marani, Livio Brasili, Luisa Lanfrancone, Carol Imbriano, Giulia Di Rocco, Silvia Franchini
Summary: The management of advanced-stage melanoma is challenging due to resistance to current therapies. Therefore, developing alternative strategies is important. Recent research has identified a potent S2R modulator (BS148) that effectively targets melanoma. Mechanistic studies revealed that BS148 activates the endoplasmic reticulum stress response and downregulates genes related to the cholesterol pathway and activates the MAPK signaling pathway. Furthermore, BS148 treatment reduces melanoma cell viability and migration in patient-derived xenograft (PDX) cells, demonstrating its potential as a promising therapeutic target for cancer treatment.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Francesco Basoccu, Federico Cuccu, Pietro Caboni, Lidia De Luca, Andrea Porcheddu
Summary: The synthesis of nitrogen-based heterocycles is crucial for pharmaceutical and agricultural development. However, current methods often involve harsh conditions or the use of toxic solvents and reagents. Mechanochemistry offers a promising solution by reducing environmental impact. In this study, we propose a new mechanochemical protocol that utilizes thiourea dioxide to synthesize various heterocyclic moieties, providing a more sustainable and eco-friendly approach.
Article
Biochemistry & Molecular Biology
Roberta Listro, Giorgio Milli, Angelica Pellegrini, Chiara Motta, Valeria Cavalloro, Emanuela Martino, Johannes Kirchmair, Giampiero Pietrocola, Daniela Rossi, Pasquale Linciano, Simona Collina
Summary: In this study, tryptophan fluorescence spectroscopy (TFS) was used to identify potential LsrK ligands from a chemical library. Three secondary metabolites were found to effectively bind to LsrK and induce conformational changes. Molecular docking results validated the findings and showed the specific mode of interaction. The identified compounds were also found to inhibit biofilm formation in some Staphylococcus spp.
Article
Chemistry, Multidisciplinary
Francesco Basoccu, Federico Cuccu, Andrea Porcheddu
Summary: Nitroso derivatives with unique characteristics have been extensively studied in various fields, including biology and clinical research. This study demonstrates a mechanochemical procedure for synthesizing nitroso compounds under solid-state conditions and successfully synthesizes previously unknown compounds with potential biological and pharmaceutical applications.
Article
Biochemistry & Molecular Biology
Nicoletta Marchesi, Pasquale Linciano, Lucrezia Irene Maria Campagnoli, Foroogh Fahmideh, Daniela Rossi, Giosue Costa, Francesca Alessandra Ambrosio, Annalisa Barbieri, Simona Collina, Alessia Pascale
Summary: In this study, the researchers found a strong association between HuD and several nervous system diseases through an interaction network analysis. They focused on the relationship between HuD and BDNF, and discovered that folic acid can regulate BDNF expression by modulating HuD. These findings suggest that BDNF could be a therapeutic target for neurological and psychiatric diseases, and folic acid may act as an epigenetic modulator.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Giacomo Rossino, Emanuela Marchese, Giovanni Galli, Francesca Verde, Matteo Finizio, Massimo Serra, Pasquale Linciano, Simona Collina
Summary: Peptides have the potential to be potent, selective, and safe therapeutical agents and have reshaped the pharmaceutical landscape. However, traditional peptide synthesis processes are environmentally draining and require sustainable alternatives. This review discusses the importance of applying green chemistry principles to peptide synthesis for achieving a green transition era in the pharmaceutical field.
Article
Chemistry, Medicinal
Serena Della Volpe, Roberta Listro, Francesca Alessandra Ambrosio, Martina Garbagnoli, Pasquale Linciano, Daniela Rossi, Giosue Costa, Stefano Alcaro, Francesca Vasile, Anna K. H. Hirsch, Simona Collina
Summary: RNA binding protein HuR plays a role in the regulation of oncogenes and tumor suppressor genes, and its dysregulation is associated with cancer. This study utilized protein-templated dynamic combinatorial chemistry to search for novel HuR ligands that can interfere with the HuR-RNA complex. Several compounds were identified and shown to effectively interfere with HuR-RNA binding, indicating their potential as anticancer agents targeting HuR-RNA interactions.
ACS MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Giacomo Rossino, Annamaria Marra, Roberta Listro, Marco Peviani, Elena Poggio, Daniela Curti, Giorgia Pellavio, Umberto Laforenza, Giulio Dondio, Dirk Schepmann, Bernhard Wuensch, Martina Bedeschi, Noemi Marino, Anna Tesei, Hee-Jin Ha, Young-Ho Kim, Jihyae Ann, Jeewoo Lee, Pasquale Linciano, Marcello Di Giacomo, Daniela Rossi, Simona Collina
Summary: Neuropathic pain (NP) is a chronic condition caused by damaged pain-signaling pathways, affecting 10% of the world's population. Non-opioid pain-relieving drugs are urgently needed due to the risks associated with opioid analgesics. This study focused on sigma-1 receptor (S1R) antagonists and evaluated their efficacy in alleviating NP using in vitro and in vivo experiments. The compound (R/S)-RC-752 showed high affinity for S1R, functional antagonist activity, and demonstrated antinociceptive effects in animal models of NP.
Review
Chemistry, Multidisciplinary
Nicolas Fantozzi, Jean-Noel Volle, Andrea Porcheddu, David Virieux, Felipe Garcia, Evelina Colacino
Summary: This article highlights the significance of green chemistry methods for promoting sustainable development, with a focus on batch and continuous mechanochemical methods in organic synthesis. The environmentally-friendly aspects of these methods are objectively assessed using green metrics and indicators, providing a comprehensive evaluation of their greenness. The article also provides an introduction to the topic, discusses variables influencing reaction outcomes, and offers an outlook for future research in this field.
CHEMICAL SOCIETY REVIEWS
(2023)