ChemistryOpen最新文献_第4页

Glycosylation of an N-Acetylated Glucosamine Disaccharide Using an Orthogonally Protected 3-Iodo-Kdo Fluoride Donor. 使用正交保护的3-碘- kdo氟给体的n -乙酰化氨基葡萄糖二糖的糖基化。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-14 DOI: 10.1002/open.202500141

Takaaki Goto, Markus Blaukopf, Berthold Stöger, Ralph Pantophlet, Lukáš Kerner, Paul Kosma

引用次数: 0

Evaluation of Benzo[cd]indol-2(1H)-ones as Downstream Hedgehog Pathway Inhibitors

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-14 DOI: 10.1002/open.202500119

Dr. Ioannis A. Tsakoumagkos, Quentin T. L. Pasquer, Christian-Louis Guillod, Dr. Charlotte Rossion, Dr. Meropi Bagka, Sonya Torche, Dr. Tomoyo Sakata-Kato, Prof. Dr. James K. Chen, Prof. Dr. Sascha Hoogendoorn

{"title":"Evaluation of Benzo[cd]indol-2(1H)-ones as Downstream Hedgehog Pathway Inhibitors","authors":"Dr. Ioannis A. Tsakoumagkos, Quentin T. L. Pasquer, Christian-Louis Guillod, Dr. Charlotte Rossion, Dr. Meropi Bagka, Sonya Torche, Dr. Tomoyo Sakata-Kato, Prof. Dr. James K. Chen, Prof. Dr. Sascha Hoogendoorn","doi":"10.1002/open.202500119","DOIUrl":"https://doi.org/10.1002/open.202500119","url":null,"abstract":"Epigenetic targeting of the Hedgehog (HH) signaling pathway has emerged as a possible strategy to combat HH pathway-driven cancers. In this study, we report on benzo[cd]indol-2(1H)-ones as downstream Hedgehog pathway inhibitors. We find that benzo[cd]indol-2(1H)-one 1 has sub-micromolar potency in a variety of Hedgehog pathway cell models, including those with constitutive activity through loss of Suppressor of Fused. Compound 1 furthermore reduces cellular and ciliary GLI levels, and, like the BET bromodomain inhibitor HPI-1, increases the cellular levels of BRD2. To directly assess the ability of compound 1 to bind to BET bromodomains in cells without the need of synthetic modifications, we develop a competition assay against degrader HPP-9, the action of which was dose-dependently outcompeted by compound 1. Indeed, compound 1 reduces the viability of GLI-driven lung cancer cells and medulloblastoma spheroids, with a potency similar to its inhibitory effect on the HH pathway. Taken together, our studies highlight the potential of the benzo[cd]indol-2(1H)-one scaffold for epigenetic targeting of the HH pathway.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":"14 5","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/open.202500119","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143944744","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Triaminoalkenes Derived from Cyclic (Alkyl)(amino)carbenes with a 1,1'-Ferrocenylene Backbone and N-Heterocyclic Carbenes: fcCAAC-NHC Heterodimers. 以1,1'-二茂铁为骨架的环（烷基）（氨基）碳烯和n -杂环碳烯衍生的三胺烯烃：fcCAAC-NHC异二聚体。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-14 DOI: 10.1002/open.202500156

Suman Yadav, Clemens Bruhn, Clemens Lücke, Richard Rudolf, Tabea Pfister, Biprajit Sarkar, Ulrich Siemeling

{"title":"Triaminoalkenes Derived from Cyclic (Alkyl)(amino)carbenes with a 1,1'-Ferrocenylene Backbone and N-Heterocyclic Carbenes: fcCAAC-NHC Heterodimers.","authors":"Suman Yadav, Clemens Bruhn, Clemens Lücke, Richard Rudolf, Tabea Pfister, Biprajit Sarkar, Ulrich Siemeling","doi":"10.1002/open.202500156","DOIUrl":"https://doi.org/10.1002/open.202500156","url":null,"abstract":"The study addresses triaminoalkenes derived from [3]ferrocenophane-type cyclic (alkyl)(amino)carbenes (fcCAACs) fc(CPh2CNR) (fc = 1,1'-ferrocenylene) and N-heterocyclic carbenes (NHCs). Stable target compounds are obtained in good yields as crystalline solids by the combination of [fc(CPh2CHNMe)][BF4] with N,N'-dimethylimidazolin-2-ylidene and of [fc(CPh2CHN-p-C6H4-tBu)](OTf) with 1,3,4,5-tetramethylimidazolin-2-ylidene, respectively, followed by treatment of the resulting addition product with KN(SiMe3)2. Due to the presence of a triaminoethene unit and a ferrocene moiety, four redox states are expected for such fcCAAC-NHC heterodimers, viz., electroneutral, mono-, di-, and tricationic. An investigation of their redox behavior by electrochemical methods (cyclic voltammetry and differential pulse voltammetry) has revealed that these compounds undergo two consecutive one-electron oxidations, with the poor stability of the dicationic species in solution preventing an observation of the tricationic redox state. A density functional theory (DFT) study shows that the highest occupied molecular orbital (HOMO) is localized on the CCN2 atom, which, in agreement with electron paramagnetic resonance results, is the site of the first oxidation. The second oxidation mainly involves the Fe atom, where the HOMO-1 is localized, resulting in a species with a triplet ground state composed, to a first approximation, of a carbon-centered and an iron-centered radical.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500156"},"PeriodicalIF":2.5,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143966941","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Analysis of Interactions Between Pyomelanin and the Extracellular Matrix in an Ex Vivo Turkey Tendon Model. 体外火鸡肌腱模型中黑色素与细胞外基质相互作用的分析。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-13 DOI: 10.1002/open.202500194

Rebecca F Shepherd, Hanaa A Galeb, Jade Bentham, Reza Moshrefi, Katelyn Ryan, Nur A B C A Tantowi, Sara J Baldock, Nathan R Halcovitch, T Jane Stockmann, John G Hardy, Jemma G Kerns, Adam M Taylor

{"title":"Analysis of Interactions Between Pyomelanin and the Extracellular Matrix in an Ex Vivo Turkey Tendon Model.","authors":"Rebecca F Shepherd, Hanaa A Galeb, Jade Bentham, Reza Moshrefi, Katelyn Ryan, Nur A B C A Tantowi, Sara J Baldock, Nathan R Halcovitch, T Jane Stockmann, John G Hardy, Jemma G Kerns, Adam M Taylor","doi":"10.1002/open.202500194","DOIUrl":"https://doi.org/10.1002/open.202500194","url":null,"abstract":"Melanins are conjugated biopolymers with varying compositions and functions, found in various tissues throughout the body. Here, the conjugated polymers derived from homogentisic acid (HGA), polyHGA (a simplified model of pyomelanin), formed in an ex vivo tendon model are examined with a view to understanding interactions between melanins and the extracellular matrix (ECM) using a selection of different analytical techniques, including spectroscopy (energy dispersive X-ray, infrared, and Raman), X-ray diffraction, and microscopy (electron, optical, and scanning electrochemical). The combination of techniques was used to facilitate an understanding of subtle differences in the composition and distribution of ECM components, hydroxyapatite, and melanin in the tendons for the first time. PolyHGA deposition in connective tissues in patients with alkaptonuria is a significant burden and causes multiple tendon ruptures due to the significant alterations in collagen properties. A similar pathology is seen in the wider population from calcific tendinitis because of hydroxyapatite crystal deposition in tendons of the shoulder and lower limbs, in particular.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500194"},"PeriodicalIF":2.5,"publicationDate":"2025-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143978873","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Flexible Screen-Printed Electrochemical Sensor for Alkaline Phosphatase Detection in Biofluids for Biomedical Applications. 用于生物医学应用的生物流体中碱性磷酸酶检测的柔性丝网印刷电化学传感器。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-13 DOI: 10.1002/open.202500113

Panagiota M Kalligosfyri, Antonella Miglione, Alessia Esposito, Raghad Alhardan, Gabriella Iula, Iclal Atay, Ibrahim A Darwish, Sevinc Kurbanoglu, Stefano Cinti

{"title":"Flexible Screen-Printed Electrochemical Sensor for Alkaline Phosphatase Detection in Biofluids for Biomedical Applications.","authors":"Panagiota M Kalligosfyri, Antonella Miglione, Alessia Esposito, Raghad Alhardan, Gabriella Iula, Iclal Atay, Ibrahim A Darwish, Sevinc Kurbanoglu, Stefano Cinti","doi":"10.1002/open.202500113","DOIUrl":"https://doi.org/10.1002/open.202500113","url":null,"abstract":"Alkaline phosphatase (ALP) is an enzyme present in the human body responsible for the dephosphorylation of phosphorylated chemical species. It is primarily expressed in organs such as bones, liver, intestine, and placenta during pregnancy, playing a crucial role in cellular processes like gene expression, transport, and metabolism. Physiological ALP levels vary with age and sex, with normal serum ranges for healthy adults between 40 and 190 U/L. Alterations in ALP levels can be indicative of several pathologies, including cancer diagnosis and metastasis, as well as bone growth dysfunctions and hypophosphatasia. Conventional methods for ALP detection often require complex assay principles, extensive sample pretreatment, and trained personnel. Herein, the development of a portable, flexible electrochemical sensor fabricated through screen-printing to monitor ALP levels in biological samples is introduced. The flexible electrochemical sensor, characterized by high efficiency, sustainability, low cost, and ease of disposal, achieves detection limit as low as 0.03 and 0.08 U/L, respectively, in buffer solution and human serum samples, and a satisfactory repeatability lower than 10%. This simple sensor configuration approach enables real-time disease monitoring and improves access to point-of-care diagnostics, paving the way for affordable, decentralized sensors that support early diagnosis and better healthcare.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500113"},"PeriodicalIF":2.5,"publicationDate":"2025-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143984869","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Development of n-type ZnAlInO Semiconductor Materials for Thermoelectric Generators in Aerospace Applications. 航空热电发电机用n型zno半导体材料的研制。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-13 DOI: 10.1002/open.202500082

Enes Kilinc, Fatih Uysal, Mucahit Abdullah Sari, Huseyin Kurt, Erdal Celik

{"title":"Development of n-type ZnAlInO Semiconductor Materials for Thermoelectric Generators in Aerospace Applications.","authors":"Enes Kilinc, Fatih Uysal, Mucahit Abdullah Sari, Huseyin Kurt, Erdal Celik","doi":"10.1002/open.202500082","DOIUrl":"https://doi.org/10.1002/open.202500082","url":null,"abstract":"Thermoelectric conversion is a system that can convert heat energy originating from temperature difference into electrical energy. Although it has many advantages in terms of usage, research is required to acquire high-efficiency thermoelectric materials due to their low efficiency. Herein, Al- and In-doped ZnO semiconductor thermoelectric material is synthesized, produced, and examined for use in the production of thermoelectric generators that can be used in aviation applications. The synthesis of ZnAlIn powders is carried out by the sol-gel method. The xerogel is dried at 200 °C for 10 h, and the dried material is then calcined at 600 °C for 4 h in an atmospheric oven to obtain ZnAlIn material. The obtained powder is then compressed with a cold press to produce pellet samples. Pellet samples are sintered in an atmospheric furnace at 1350 °C for 36 h and are made ready for measurements. Comprehensive characterization and analysis of microstructural and structural properties are performed by Fourier transform infrared spectroscopy, differential thermal analysis-thermogravimetry, X-ray photoelectron spectroscopy, scanning electron microscopy, and X-ray diffraction methods. Seebeck coefficient and thermal capacity measurements are performed to determine thermoelectric properties. The results obtained from the study show that ceramic-based ZnAlIn semiconductor thermoelectric material has the required efficiency for thermoelectric generator production.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500082"},"PeriodicalIF":2.5,"publicationDate":"2025-04-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143974555","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effects of Catalyst Synthesis Methods on the Physicochemical Properties of Silica-Supported Au-Ru Bimetallic Catalysts and their Influence on the Oxidation of Phenols with H₂O₂. 催化剂合成方法对二氧化硅负载金钌双金属催化剂理化性质的影响及其对H2O2氧化苯酚的影响

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-10 DOI: 10.1002/open.202400484

Tumisang Lekgetho, Matshawandile Tukulula, Letlhogonolo Fortunate Mabena, Mabuatsela Virginia Maphoru

{"title":"Effects of Catalyst Synthesis Methods on the Physicochemical Properties of Silica-Supported Au-Ru Bimetallic Catalysts and their Influence on the Oxidation of Phenols with H2O2.","authors":"Tumisang Lekgetho, Matshawandile Tukulula, Letlhogonolo Fortunate Mabena, Mabuatsela Virginia Maphoru","doi":"10.1002/open.202400484","DOIUrl":"https://doi.org/10.1002/open.202400484","url":null,"abstract":"Herein, silica-supported Au-Ru catalysts with 5% loading for each metal were prepared by microwave-assisted loading (MW) and deposition (DP) methods. Au-Ru nanoparticles are obtained on MW-5Au5Ru while short Au-Ru nanochains are obtained on DP-5Au5Ru. The performance of the catalysts is tested through the oxidation of 2,3,5-trimethylhydroquinone (TMHQ) and 4-methoxy-1-naphthol (MNL) with H2O2, in which 2,3,5-trimethyl-1,4-benzoquinone (TMBQ) and 4,4'-dimethoxy-2,2'-binaphthalenylidene-1,1'-dione (BNP) are produced as main products, respectively. Catalytic data obtained for the oxidation of TMHQ demonstrate that the structures of the catalysts, type of solvent, and reaction temperatures used have a significant influence on the activities and selectivities of the catalysts. When MeOH and MeNO2 are used at room temperature (RT) in the oxidation of TMHQ on MW-5Au5Ru catalyst, 58.2% and 100% conversions of TMHQ are achieved, respectively. Both MW and DP-synthesized catalysts are highly active in the oxidation of TMHQ. Similar to TMHQ, the catalytic outcomes on the oxidative coupling of MNL highly depend on the temperature and structure of the catalyst. For example, 34% and 96% conversions of MNL are achieved at RT and 60 °C, respectively, over MW-5Au5Ru catalyst in MeOH. However, MNL conversion of 82% is achieved on DP-5Au5Ru catalyst in MeOH at RT.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2400484"},"PeriodicalIF":2.5,"publicationDate":"2025-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143961467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Preparation of P-Doped Ni Catalyst Using Deep Eutectic Solvents and Its Excellent Hydrogen Evolution Performance in Water Splitting. 用深共晶溶剂制备p掺杂Ni催化剂及其在水裂解中优异的析氢性能。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-10 DOI: 10.1002/open.202500023

Chenyun Zhang, Jiahao Wang

{"title":"Preparation of P-Doped Ni Catalyst Using Deep Eutectic Solvents and Its Excellent Hydrogen Evolution Performance in Water Splitting.","authors":"Chenyun Zhang, Jiahao Wang","doi":"10.1002/open.202500023","DOIUrl":"https://doi.org/10.1002/open.202500023","url":null,"abstract":"A deep eutectic solvent (DES) was prepared by mixing tetraalkylphosphonium chloride ([P4444]Cl) and glycerol in a 1:2 molar ratio. Nickel nitrate was dissolved in this DES, and then the mixture was heated at 350 °C to obtain phosphorus-doped nickel catalysts. In this system, the DES plays multiple crucial roles. (1) It serves as a reaction medium, providing a suitable solvent environment for the synthesis of Ni-based catalysts. (2) It actively participates in the catalyst preparation as a reactant. [P4444]Cl acts as a P source, while glycerol effectively promotes the formation of nickel metal as a reducing agent. (3) It exhibits a templating effect, inducing the morphology of product to be a unique thin sheet with angular edges. The synthesized P-doped Ni material exhibits excellent hydrogen evolution performance in water splitting. In an acidic environment, when the current densities reached 10 and 20 mA cm-2, the overpotentials were only 90.2 and 115.9 mV, with a Tafel slope as low as 55.6 mV dec-1. In an alkaline environment, the P-doped Ni also performed well. The η10 and η20 values were 107.0 and 145.4 mV, respectively. The Tafel slope was 57.0 mV dec-1.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500023"},"PeriodicalIF":2.5,"publicationDate":"2025-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143955135","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pd-Catalyzed Cross-Coupling of Alkylbisboronic Esters. 钯催化烷基双硼酯的交叉偶联。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-10 DOI: 10.1002/open.202500195

Philip P Scott, Christopher E Baird, Elizabeth A Kraichely, Liam M Radeke, Timothy J Barker

引用次数: 0

Studies Concerned with the Structure and Synthesis of the Anti-viral Tropolone Glycoside Liriosmaside A. 抗病毒Tropolone糖苷liriosm苷A的结构与合成研究。

IF 2.5 4区化学

ChemistryOpen Pub Date : 2025-04-08 DOI: 10.1002/open.202500011

Qi Chen, Yaping Zhan, Michael G Gardiner, Zeinab G Khalil, Amila A Dewa, Thulasi Sritharan, Robert J Capon, Ping Lan, Shen Tan, Martin G Banwell

{"title":"Studies Concerned with the Structure and Synthesis of the Anti-viral Tropolone Glycoside Liriosmaside A.","authors":"Qi Chen, Yaping Zhan, Michael G Gardiner, Zeinab G Khalil, Amila A Dewa, Thulasi Sritharan, Robert J Capon, Ping Lan, Shen Tan, Martin G Banwell","doi":"10.1002/open.202500011","DOIUrl":"https://doi.org/10.1002/open.202500011","url":null,"abstract":"A bromotropone corresponding to the agylcone of the glycosylated sesquiterpenoid natural product liriosmaside A has been prepared over ten steps and in a fully regio-controlled manner through the gem-dibromocyclopropane-mediated ring-expansion of a readily accessible decalenone. A Pd[0]-mediated glucosylation reaction applied to this bromotropone afforded a product mixture from which an enantiomerically pure cross-coupling product could be obtained and its structure confirmed through single-crystal X-ray analysis of a derivative. Various (unsuccessful) attempts are described to selectively acylate the last compound and thereby install the 3-hydroxy-3-methylglutaric acid or HMGA-containing side chain of the title natural product. A literature survey of other natural products embodying the HMGA motif suggest that liriosmaside A and its co-metabolite liriosmaside B could be S-configured at C3\". The evaluation of the glucosylated tropone in a series of anti-bacterial, anti-fungal and cytotoxicity assays reveals that it is inactive in all of these and so emphasizing the prospect that this and related troponoids, including the natural products liriosmaside A and B, can serve as useful models for new anti-viral agents.","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e202500011"},"PeriodicalIF":2.5,"publicationDate":"2025-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143810650","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0