ChemistryOpen最新文献

筛选
英文 中文
Green Synthesis and Application of Biochar Derived from Alien Vegetation Wood for Proton Exchange Membrane Fuel Cells. 外来植被木材生物炭的绿色合成及其在质子交换膜燃料电池中的应用。
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-26 DOI: 10.1002/open.202500025
Alunge Gift Sobekwa, Nakedi Albert Mojapelo, Evan David Visser, Ntalane Sello Seroka, Lindiwe Khotseng
{"title":"Green Synthesis and Application of Biochar Derived from Alien Vegetation Wood for Proton Exchange Membrane Fuel Cells.","authors":"Alunge Gift Sobekwa, Nakedi Albert Mojapelo, Evan David Visser, Ntalane Sello Seroka, Lindiwe Khotseng","doi":"10.1002/open.202500025","DOIUrl":"https://doi.org/10.1002/open.202500025","url":null,"abstract":"<p><p>Invasive alien vegetation brought about by various human activities has grown to be a significant threat to the ecosystem and its diversity; therefore, control strategies to combat this threat are being explored. This review aims to investigate the prospect of using biochar specifically from alien vegetation as a support material for the proton exchange membrane (PEM) fuel cell electrocatalyst, highlighting the need to move to green energy and invest in Eco conservation. The use of biochar derived from alien vegetation as carbon support for the platinum (Pt) electrocatalyst for PEM fuel cells is an interesting field that is slowly gaining momentum. Biochar has the potential to be used as a carbon support due to its high specific surface, area, and intrinsic property needed for an electrocatalyst support. The current widely used electrocatalyst, which is Pt supported on carbon black, has shown to suffer from corrosion which weakens the bond between the support and the Pt nanoparticles, leading to instability and resistance; therefore, alternative supports are needed also to decrease the Pt loading as it is expensive. The focus of this review is on the benefits and prospects of these cheap green resources in increasing efforts to conserve the environment.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500025"},"PeriodicalIF":2.5,"publicationDate":"2025-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143983643","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 G–Ag and C–Ag Nanoparticle-Based Biosensor for Benzoic Acid Detection 基于G-Ag和C-Ag纳米粒子的苯甲酸检测生物传感器的研制
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-24 DOI: 10.1002/open.202400418
Mehmet Selcuk Erdogan, Muhammed Bekmezci, Nihal Yigit Ertas, Ramazan Bayat, Fatih Sen
{"title":"Development of G–Ag and C–Ag Nanoparticle-Based Biosensor for Benzoic Acid Detection","authors":"Mehmet Selcuk Erdogan,&nbsp;Muhammed Bekmezci,&nbsp;Nihal Yigit Ertas,&nbsp;Ramazan Bayat,&nbsp;Fatih Sen","doi":"10.1002/open.202400418","DOIUrl":"10.1002/open.202400418","url":null,"abstract":"<p>In this study, an efficient electrochemical sensor for the highly sensitive detection of benzoic acid (BA) is developed using silver nanoparticles (Ag NPs) obtained by two different methods: the green synthesis method (G–Ag) and the chemical synthesis method (C–Ag). Linden flower extract is prepared and used for the biosynthesis of Ag NPs. Sodium borohydride, NaBH<sub>4</sub>, is used as a reducing agent in chemical synthesis. Ag NPs are characterized by the X-ray diffraction (XRD) method, scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, and UV-visible spectrometry. According to the XRD results, the crystal sizes for G–Ag and C–Ag are calculated to be 24.07 and 5.91 nm, respectively. G–Ag and C–Ag NP-modified glassy carbon electrodes (GCEs) and cyclic voltammetry (CV) and differential pulse voltammetry (DPV) are used as electrochemical methods to determine BA. The limits of detection of G–Ag and C–Ag NP-modified GCEs are calculated as 1.67 mM limit of quantification and 10 mM, respectively. The linear ranges of GCEs modified with nanomaterials are determined as 2.40–8.01 mM for C–Ag and 4.84–14.66 mM for G–Ag. The study is significant in that the NPs obtained by the biological synthesis method showed as good activity as the particles synthesized by the chemical method.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":"14 6","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/open.202400418","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143969304","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
Dry Coating with Hydrophilic and Hydrophobized Nanostructured Fumed Alumina (Al2O3) on SiOx/C Anodes for Enhanced Lithium-Ion Battery Performance. 亲水和疏水纳米结构气相氧化铝(Al2O3)在SiOx/C阳极上的干涂层提高锂离子电池性能。
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-21 DOI: 10.1002/open.202500170
Ana L Azevedo Costa, Daniel Esken, Tatiana Gambaryan-Roisman, Frank Menzel
{"title":"Dry Coating with Hydrophilic and Hydrophobized Nanostructured Fumed Alumina (Al<sub>2</sub>O<sub>3</sub>) on SiO<sub>x</sub>/C Anodes for Enhanced Lithium-Ion Battery Performance.","authors":"Ana L Azevedo Costa, Daniel Esken, Tatiana Gambaryan-Roisman, Frank Menzel","doi":"10.1002/open.202500170","DOIUrl":"https://doi.org/10.1002/open.202500170","url":null,"abstract":"<p><p>Silicon-based anode materials hold great promise for advancing lithium-ion battery technology due to their high specific capacity, low voltage platform, abundant resources, and environmental benefits. However, their inherent challenges, such as poor electrical conductivity, significant volume expansion, and instability of the solid-electrolyte interphase layer, hinder their widespread commercialization. This study addresses these issues using the dry particle coating method with nanostructured fumed aluminum oxide (Al<sub>2</sub>O<sub>3</sub>), a novel approach with significant potential for commercial scalability. The impact of surface wettability on performance is studied by applying metal oxide coatings, using hydrophilic and hydrophobized surfaces. Electrochemical evaluation shows a significant increase in rate performance and cycle life when the surface coating is applied, with improvements in discharge capacity of around 10% and 17% for hydrophobized and hydrophilic Al<sub>2</sub>O<sub>3</sub> coatings, respectively, after 100 cycles. The Al<sub>2</sub>O<sub>3</sub> coating protects the surface of the active material, preventing particle pulverization, reducing side reactions, and decreasing electrolyte decomposition and hydrofluoric acid content. While overall performance improves with coating, the best results are achieved with the hydrophilic coating, which fosters a more homogeneous microstructured electrode. These findings underscore the potential of the dry particle coating technique with Al<sub>2</sub>O<sub>3</sub> to enhance Si-based anode performance and facilitate commercial application.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500170"},"PeriodicalIF":2.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143984895","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
Synthesis of Fe3O4@Au Core-Shell Nanoparticles with Varying Thicknesses for Application in Computed Tomography Imaging. 合成Fe3O4@Au不同厚度核壳纳米颗粒在计算机断层成像中的应用。
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-21 DOI: 10.1002/open.202500166
Nguyen Thi Ngoc Linh, Nguyen Hoa Du, Ngo Thanh Dung, Le Thi Thanh Tam, Pham Hong Nam, Phan Thi Hong Tuyet, Le Trong Lu, Le The Tam
{"title":"Synthesis of Fe<sub>3</sub>O<sub>4</sub>@Au Core-Shell Nanoparticles with Varying Thicknesses for Application in Computed Tomography Imaging.","authors":"Nguyen Thi Ngoc Linh, Nguyen Hoa Du, Ngo Thanh Dung, Le Thi Thanh Tam, Pham Hong Nam, Phan Thi Hong Tuyet, Le Trong Lu, Le The Tam","doi":"10.1002/open.202500166","DOIUrl":"https://doi.org/10.1002/open.202500166","url":null,"abstract":"<p><p>To enhance the resolution of medical images, core-shell Fe<sub>3</sub>O<sub>4</sub>@Au hybrid nanoparticles (HNPs) with gold shells of varying thicknesses are developed. By optimizing synthesis conditions, nanoparticles with uniform size, clear core-shell structure, and high stability in biological environments are obtained. In vitro testing data shows that HNPs with a 5-7 nm-thick gold shell exhibits a high X-ray attenuation. The in vivo efficacy of the Fe<sub>3</sub>O<sub>4</sub>@Au HNPs is tested in liver and kidney tissues in a mouse model for study on drug kinetics. Results demonstrate the effectiveness of Fe<sub>3</sub>O<sub>4</sub>@Au HNPs in enhancing the contrast of computed tomography (CT) images, especially in the liver. Simultaneously, the clearance process of nanoparticles through the kidneys is also observed, opening up the prospect of applying these nanoparticles in image diagnosis and treatment monitoring. Overall, these hybrid particles are a promising candidate for CT imaging techniques.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500166"},"PeriodicalIF":2.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143955804","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
One-Step Aqueous Synthesis of Glycosyl Pyridinium Salts, Electrochemical Study, and Assessment of Utility as Precursors of Glycosyl Radicals Using Photoredox Catalysis. 一步水法合成糖基吡啶盐,电化学研究及光氧化还原催化作为糖基自由基前体的效用评价。
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-21 DOI: 10.1002/open.202500183
Daniel Chong, Paula A Brooksby, Antony J Fairbanks
{"title":"One-Step Aqueous Synthesis of Glycosyl Pyridinium Salts, Electrochemical Study, and Assessment of Utility as Precursors of Glycosyl Radicals Using Photoredox Catalysis.","authors":"Daniel Chong, Paula A Brooksby, Antony J Fairbanks","doi":"10.1002/open.202500183","DOIUrl":"https://doi.org/10.1002/open.202500183","url":null,"abstract":"<p><p>A single step method for the production of unprotected glycosyl pyridinium salts has been developed involving treatment of the unprotected sugar with a pyridine, triethylamine, and either 2-chloro-1,3-dimethylimidazolinium chloride (DMC) or 2-chloro-1,3-dimethyl-1 H-benzimidazol-3-ium chloride (CDMBI) as an activator, in aqueous solution. Reaction efficiency is sensitive to steric effects, and in particular, ortho-substitution of the pyridine ring significantly decreased conversion to product; para-substitution of the pyridine ring is well tolerated. Cyclic voltammetry reveals that glycosyl pyridinium salts possess reduction potentials in the range of -0.9 to -1.4 V versus the standard calomel electrode, which are modulated by the electron effects of ring substituents. However, glycosyl pyridiniums are not found to be useful precursors for the production of glycosyl radicals under photoredox conditions.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500183"},"PeriodicalIF":2.5,"publicationDate":"2025-04-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143978776","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
Unveiling the Therapeutic Potential of Atractylis aristata Batt. Aqueous Extract: Anti-inflammatory, Antioxidant, Antibacterial, Sedative Activities & Phytochemical Profiling. 揭示白术的治疗潜力。水提取物:抗炎,抗氧化,抗菌,镇静活性和植物化学分析。
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-17 DOI: 10.1002/open.202500056
Asma Abid, Nourelhouda Mekhadmi, Randa Mlik, Assia Bentahar, Kamilia Bireche, Bariza Frih, Walid Boussebaa, Aicha Mouane, Nezar Cherrada, Ana Sanches Silva, Messaouda Dekmouche, Lazhar Bechki, Khalid Mashay Al-Anazi, Mohammad Abul Farah, Ahmad Ali
{"title":"Unveiling the Therapeutic Potential of Atractylis aristata Batt. Aqueous Extract: Anti-inflammatory, Antioxidant, Antibacterial, Sedative Activities & Phytochemical Profiling.","authors":"Asma Abid, Nourelhouda Mekhadmi, Randa Mlik, Assia Bentahar, Kamilia Bireche, Bariza Frih, Walid Boussebaa, Aicha Mouane, Nezar Cherrada, Ana Sanches Silva, Messaouda Dekmouche, Lazhar Bechki, Khalid Mashay Al-Anazi, Mohammad Abul Farah, Ahmad Ali","doi":"10.1002/open.202500056","DOIUrl":"https://doi.org/10.1002/open.202500056","url":null,"abstract":"<p><p>Medicinal plants possess the potential to yield bioactive compounds that offer significant health benefits; positioning them as valuable and promising sources for the development of innovative pharmaceutical products. This study aims to comprehensively assess the in vitro and in vivo pharmacological effects of the aqueous extract of the plant Atractylis aristata (AEAA) as well as assessments of its phytochemical composition. UPLC-ESI-MS/MS analysis of AEAA revealed a variety of bioactive compounds, including flavonoids and phenolic acids. In antioxidant assays, AEAA demonstrated considerable activity, with IC<sub>50</sub> values of 0.269±0.05 mg/mL for DPPH scavenging and 0.0376±0.003 mg/mL for hydrogen peroxide radical inhibition. AEAA exhibited strong anti-inflammatory activity in vitro, with an IC<sub>50</sub> value of 2.563 mg/mL in the BSA denaturation test. In vivo, AEAA reduced carrageenan-induced paw edema by 56.51 %, in comparison to an 83.58 % reduction with Ibuprofen®. Antibacterial testing showed AEAA's broad-spectrum activity, with the highest inhibition against Bacillus subtilis (34 mm zone of inhibition). Additionally, AEAA induced significant sedative effects, reducing locomotor activity by 48.98 %. These findings underscore the diverse pharmacological potential in addressing oxidative stress, inflammation, microbial infections, and anxiety of A. aristata, which can be attributed to its rich phytochemical profile.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e202500056"},"PeriodicalIF":2.5,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143966536","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
Three-Component 1,2-Methylamidation of Alkynes via Coordinating Activation Strategy. 配位活化策略下炔的三组分1,2-甲基化反应。
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-17 DOI: 10.1002/open.202500151
Jing Ren, Kaiyun Liu, Ning Wang, Jinlong Li, Xinyu Long, Chengming Li, Kaizhi Li
{"title":"Three-Component 1,2-Methylamidation of Alkynes via Coordinating Activation Strategy.","authors":"Jing Ren, Kaiyun Liu, Ning Wang, Jinlong Li, Xinyu Long, Chengming Li, Kaizhi Li","doi":"10.1002/open.202500151","DOIUrl":"https://doi.org/10.1002/open.202500151","url":null,"abstract":"<p><p>The selective functionalization of carbon-carbon triple bonds with methyl groups remains a challenging task. Herein, the successful development of a novel copper-catalyzed three-component 1,2-methylamidation of carbon-carbon triple bond is reported. The readily available coupling partners, picolinamides and alkynes with dicumyl peroxide, serve as both the methyl source and oxidant in this difunctional strategy to access methylated enamides; the substrate scope is broad, demonstrating good functional group compatibility. The synthetic utility of the reaction is also demonstrated through the 1,2-methylamidation of alkynes via late-stage functionalization of substrates bearing biologically relevant molecules.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500151"},"PeriodicalIF":2.5,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143992560","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
Go for Gold: Development of a Scalable Synthesis of [1-(Ethoxycarbonyl)cyclopropyl] Triphenylphosphonium Tetrafluoroborate, a Key Reagent to Explore Covalent Monopolar Spindle 1 Inhibitors. 寻找黄金:可扩展合成[1-(乙氧羰基)环丙基]三苯基四氟硼酸磷的开发,这是探索共价单极梭形1抑制剂的关键试剂。
IF 2.5 4区 化学
ChemistryOpen Pub Date : 2025-04-16 DOI: 10.1002/open.202500106
Leon Rebhan, Rebekka Fürst, Dieter Schollmeyer, Ricardo A M Serafim, Matthias Gehringer
{"title":"Go for Gold: Development of a Scalable Synthesis of [1-(Ethoxycarbonyl)cyclopropyl] Triphenylphosphonium Tetrafluoroborate, a Key Reagent to Explore Covalent Monopolar Spindle 1 Inhibitors.","authors":"Leon Rebhan, Rebekka Fürst, Dieter Schollmeyer, Ricardo A M Serafim, Matthias Gehringer","doi":"10.1002/open.202500106","DOIUrl":"https://doi.org/10.1002/open.202500106","url":null,"abstract":"<p><p>Covalent approaches have resurged in drug discovery and chemical biology during the last decade. So-called targeted covalent inhibitors typically show a strong and persistent drug-target interaction as well as a high degree of selectivity. In our research group, RMS-07 (8), a First-in-Class covalent inhibitor of the protein kinase threonine tyrosine kinase (TTK)/monopolar spindle 1, which shows promising results in a variety of different solid cancer cell types and will be further optimized in terms of covalent binding kinetics, has recently been developed. However, synthetic accessibility is restricted by a high price and limited availability of [1-(ethoxycarbonyl)cyclopropyl] triphenylphosphonium tetrafluoroborate (10), a key reagent required to assemble the tricyclic core scaffold in a Wittig-type cyclization reaction. This reagent is also described as a valuable synthon for the synthesis of a range of ring systems with interesting applications in medicinal chemistry. However, reliable procedures for its large-scale synthesis are scarce. Only one prior report describes the synthesis of reagent 10, and it contains limited experimental details, making it challenging to reproduce and scale up. Herein, a concise and reproducible decigram-scale synthetic protocol for accessing key reagent 10 is described.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500106"},"PeriodicalIF":2.5,"publicationDate":"2025-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143963104","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
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
{"title":"Glycosylation of an N-Acetylated Glucosamine Disaccharide Using an Orthogonally Protected 3-Iodo-Kdo Fluoride Donor.","authors":"Takaaki Goto, Markus Blaukopf, Berthold Stöger, Ralph Pantophlet, Lukáš Kerner, Paul Kosma","doi":"10.1002/open.202500141","DOIUrl":"https://doi.org/10.1002/open.202500141","url":null,"abstract":"<p><p>Kdo (3-Deoxy-d-manno-oct-2-ulosonic acid) is an essential sugar found in bacterial lipopolysaccharides with significant biomedical relevance. This study introduces an orthogonally protected 3-iodo-Kdo fluoride donor and demonstrates its coupling to a pre-synthesized β-(1→6)-linked N-acetylglucosamine disaccharide acceptor as an example. Nuclear magnetic resonance data indicates the presence of an intraresidue hydrogen bond in the distal glucosamine unit. Two complementary glycosylation approaches are explored with an emphasis on achieving high stereoselectivity and minimizing protecting-group manipulation. The orthogonal protection of 3-iodo Kdo fluoride donor offers insights into tailoring Kdo-based donors for specific biomedical applications. While yields vary depending on the approach, they are sufficient to demonstrate the donor's applicability. These findings enable the design of advanced glycomimetic constructs for therapeutic and vaccine research.</p>","PeriodicalId":9831,"journal":{"name":"ChemistryOpen","volume":" ","pages":"e2500141"},"PeriodicalIF":2.5,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143978171","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
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,&nbsp;Quentin T. L. Pasquer,&nbsp;Christian-Louis Guillod,&nbsp;Dr. Charlotte Rossion,&nbsp;Dr. Meropi Bagka,&nbsp;Sonya Torche,&nbsp;Dr. Tomoyo Sakata-Kato,&nbsp;Prof. Dr. James K. Chen,&nbsp;Prof. Dr. Sascha Hoogendoorn","doi":"10.1002/open.202500119","DOIUrl":"https://doi.org/10.1002/open.202500119","url":null,"abstract":"<p>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[<i>cd</i>]indol-2(1<i>H</i>)-ones as downstream Hedgehog pathway inhibitors. We find that benzo[<i>cd</i>]indol-2(1<i>H</i>)-one <b>1</b> has sub-micromolar potency in a variety of Hedgehog pathway cell models, including those with constitutive activity through loss of Suppressor of Fused. Compound <b>1</b> 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 <b>1</b> 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 <b>1</b>. Indeed, compound <b>1</b> 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[<i>cd</i>]indol-2(1<i>H</i>)-one scaffold for epigenetic targeting of the HH pathway.</p>","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
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信