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New 4-imino-4H-Chromeno[2,3-d]Pyrimidin-3(5H)-Amine: Synthesis, Cytotoxic Effects on Tumoral Cell Lines and in Silico ADMET Properties

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International Journal of Organic Chemistry 2024年第3期14卷 107-122页

作者： Marwa Dhiabi Sirine Karoui Mehdi Fakhfakh Souhir Abid Emmanuelle Limanton Rémy Le Guével Thierry charlier Ludovic Paquin jean-Pierre Bazureau Houcine Ammar Laboratoire de Chimie Applique: Htrocycles Corps et Polymres Facult des Sciences de Sfax Universit de Sfax Sfax Tunisie Institut des Sciences Chimiques de Rennes Universit de Rennes Campus de Beaulieu Rennes Cedex France Department of Chemistry (Science and Arts): Al Qurayat Al-Jouf University Al Jawf Saudi Arabia S2Wave Platform ScanMAT UAR CNRS Universit de Rennes Campus de Beaulieu Rennes Cedex France ImPACcell Platform Biosit SFR UMS CNRS Inserm Campus de Villejean Rennes France Institut de Recherche en Sant Environnement et Travail IRSET Inserm UMR_S Rennes France

The synthesis of new 4-imino-4H-chromeno[2,3-d]pyrimidin-3(5H)-amine in four steps including one step under microwave dielectric heating is reported. The structural identity of the synthesized compounds was established according to their spectroscopic analysis, such as FT-IR, NMR and mass spectroscopy. These new compounds were tested for their antiproliferative activities on seven representative human tumoral cell lines (Huh7 D12, Caco2, MDA-MB231, MDA-MB468, HCT116, PC3 and MCF7) and also on fibroblasts. Among them, only the compounds 6c showed micromolar cytotoxic activity on tumor cell lines (1.8 50 50 > 25 μM). Finally, in silico ADMET studies ware performed to investigate the possibility of using of the identified compound 6c as potential anti-tumor compound.

关键词： 2-Amino-4H-Chromene 4H-Chromeno[2 3-d]Pyrimidin-3(5H)-Amine Microwave Irradiation Tumoral Cell Line in Silico ADMET

Thermal response of steel framing members in open car park fires

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Frontiers of Structural and Civil Engineering 2022年第9期16卷 1071-1088页

作者： Xia YAN Marion charlier Thomas GERNAY Department of Civil and Systems Engineering Johns Hopkins UniversityBaltimoreMD 21218USA ArcelorMittal Steligence Esch-sur-Alzette 4221Luxembourg

For open car park structures,adopting a performance-based structural fire design is often justified and allowed because the fire does not reach ***,this design approach requires an accurate assessment of temperatures in structural members exposed to car *** paper describes a numerical study on the thermal exposure on steel framing members in open car park *** temperatures are computed by the coupling of computational fluid dynamics and finite element modeling,and by analytical models from the *** addition,the influence of galvanization on the steel temperature evolution is *** show that temperatures in unprotected beams and columns are influenced by the section geometry,car fire scenario,modeling approach,and use of *** slightly delays and reduces peak *** the different models,CFD-FEM(CFD:computational fluid dynamics,FEM:finite-element method)coupled models predict lower temperatures than the Hasemi model,because the latter conservatively assumes that the fire flame continuously touches the ***,the Hasemi model cannot account for the effect of reduced emissivity from galvanization on the absorbed heat *** temperature distributions obtained in the steel members can be used to complete efficient structural fire designs based on the member sections,structure layout,and use of galvanization.

关键词： open car park localized fire steel frame numerical modeling computational fluid dynamics

Mapping and analysis of a spatiotemporal H3K27ac and gene expression spectrum in pigs

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Science China(Life Sciences) 2022年第8期65卷 1517-1534页

作者： Yaling Zhu Zhimin Zhou Tao Huang Zhen Zhang Wanbo Li Ziqi Ling Tao Jiang Jiawen Yang Siyu Yang Yanyuan Xiao Carole charlier Michel Georges Bin Yang Lusheng Huang State Key Laboratory of Pig Genetic Improvement and Production Technology Jiangxi Agricultural UniversityNanchang 330045China Laboratory Animal Research Center School of Basic Medical SciencesAnhui Medical UniversityHefei 230032China Unit of Animal Genomics GIGA-Institute and Faculty of Veterinary MedicineUniversity of Liege4000 LiegeBelgium

The limited knowledge of genomic noncoding and regulatory regions has restricted our ability to decipher the genetic mechanisms underlying complex traits in pigs. In this study, we characterized the spatiotemporal landscape of putative enhancers and promoters and their target genes by combining H3K27ac-targeted Ch IP-Seq and RNA-Seq in fetal(prenatal days 74–75) and adult(postnatal days 132–150) tissues(brain, liver, heart, muscle and small intestine) sampled from Asian aboriginal Bama Xiang and European highly selected Large White pigs of both sexes. We identified 101,290 H3K27ac peaks, marking 18,521promoters and 82,769 enhancers, including peaks that were active across all tissues and developmental stages(which could indicate safe harbor locus for exogenous gene insertion) and tissue-and developmental stage-specific peaks(which regulate gene pathways matching tissue-and developmental stage-specific physiological functions). We found that H3K27ac and DNA methylation in the promoter region of the XIST gene may be involved in X chromosome inactivation and demonstrated the utility of the present resource for revealing the regulatory patterns of known causal genes and prioritizing candidate causal variants for complex traits in pigs. In addition, we identified an average of 1,124 super-enhancers per sample and found that they were more likely to show tissue-specific activity than ordinary peaks. We have developed a web browser to improve the accessibility of the results(http://***/pencode/?genome=sus Scr11).

关键词： H3K27ac ChIP-Seq RNA-Seq pig XIST complex traits

Toward diagnostic relevance of theαVβ5,αVβ3,andαVβ6 integrins in OA:expression within human cartilage and spinal osteophytes

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Bone Research 2020年第4期8卷 458-472页

作者： Edith charlier Céline Deroyer Sophie Neuville Zelda Plener Olivier Malaise Federica Ciregia Philippe Gillet Gilles Reuter Mallory Salvé Nadia Withofs Roland Hustinx Dominique de Seny Michel G.Malaise Laboratory of Rheumatology GIGA-I3CHULiègeULiègeLiègeBelgium Department of Orthopaedic Surgery CHULiègeLiègeBelgium Department of Neurosurgery CHULiègeLiègeBelgium Department of Nuclear Medicine CHULiègeLiègeBelgium

We previously reported 18FPRGD2 uptake by the coxofemoral lining,intervertebral discs and facet joint osteophytes in OA using PET/SCAN ***,the molecular mechanism by which the PRGD2 tracer interacts with joint tissues and osteophytes in OA remains *** PRGD2 ligands are expected to belong to the RGD-specific integrin family,the purpose of this study was(i)to determine which integrin complexes display the highest affinity for PRGD2-based ligands,(ii)to analyze integrin expression in relevant tissues,and(iii)to test integrin regulation in chondrocytes using OA-related stimuli to increase the levels of fibrosis and ossification *** this end,the affinity of PRGD2-based ligands for five heterodimeric integrins was measured by competition with *** situ analyses were performed in human normal *** cartilage and spinal *** were characterized by(immuno-)histological *** subunit expression was tested in chondrocytes undergoing dedifferentiation,osteogenic differentiation,and inflammatory *** integrinsαVβ5,αVβ3,andαVβ6 presented the highest affinity for PRGD2-based *** situ,the expression of these integrins was significantly increased in OA compared to normal *** osteophytes,the mean integrin expression score was significantly higher in blood vessels,fibrous areas,and cells from the bone lining than in osteocytes and cartilaginous *** vitro,the levels of integrin subunits were significantly increased during chondrocyte dedifferentiation(except forβ6),fibrosis,and osteogenic differentiation as well as under inflammatory *** conclusion,anatomical zones(such as OA cartilage,intervertebral discs,and facet joint osteophytes)previously reported to show PRGD2 ligand uptake in vivo expressed increased levels ofαVβ5,αVβ3,andβ6 integrins,whose subunits are modulated in vitro by OA-associated conditions that increase fibrosis,inflammation,and osteogenic differentiation.T

关键词： cartilage inflammation femoral

3-(Tetrazol-5-yl)-2-imino-coumarins Derivatives: Synthesis, Characterization, and Evaluation on Tumor Cell Lines

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International Journal of Organic Chemistry 2021年第1期11卷 24-34页

作者： Ali Bouattour Mehdi Fakhfakh Souhir Abid El-Gharbi Majdi Abid Ludovic Paquin Rémy Le Guevel Thierry charlier Houcine Ammar jean-Pierre Bazureau Laboratoire de Chimie Appliquée: Hétérocycles Corps Gras et Polymères Faculté des Sciences de Sfax Université de Sfax Sfax Tunisie Chemistry Department College of Science and Arts Jouf University Al Qurayyat Al Jawf KSA Institut des Sciences Chimiques de Rennes ISCR UMR CNRS 6226 Campus Beaulieu Université de Rennes 1 Bat. 10A Rennes Cedex France S2Wave Platform ScanMAT UMS 2001 CNRS Campus Beaulieu Université de Rennes 1 Bat. 10A Rennes Cedex France ImPACcell Platform SFR Biosit Bat. 8 Campus Villejean Rennes Cedex France

The first report of new 3-(tetrazol-5-yl)-2-iminocoumarin derivatives is described. The title compounds were prepared in two steps and were obtained in good yields (55-93%). They have been fully characterized by 1H, 13C NMR, FTIR, UV-Visible and HRMS. They were tested for their antiproliferative activities against six representative human tumor cell lines (Huh 7-D12, Caco2, MDA-MB231, HCT 116, PC3 and NCI-H727) and HaCat keratinocytes. Among them, compound 5e was active on HCT 116 (IC50 15 μM).

关键词： 2-Iminocoumarin Tetrazole Fluorescence Tumor Cell Lines HCT 116

Synthesis of New 2-Phenylamino-4<i>H</i>-chromene-3-carbonitrile Derivatives and Their Effects on Tumor Cell Lines and against Protein Kinases

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International Journal of Organic Chemistry 2020年第2期10卷 88-103页

作者： Ali Bouattour Mehdi Fakhfakh Souhir Abid Ludovic Paquin Rémy Le Guével Thierry charlier Sandrine Ruchaud Stéphane Bach jean-Pierre Bazureau Houcine Ammar Laboratoire de Chimie Appliquée: Hétérocycles Corps Gras et Polymères Faculté des Sciences de Sfax Université de Sfax Sfax Tunisie Département de Chimie Collège des Sciences et des Arts Université de Jouf Al Qurayyat KSA Institut des Sciences Chimiques de Rennes (ISCR) UMR CNRS 6226 Université de Rennes 1 Campus de Beaulieu Rennes France S2 Wave Platform ScanMAT UMS 2001CNRS Université de Rennes 1 Campus de Beaulieu Rennes France Université de Rennes 1 ImPACcell Platform Campus Villejean Rennes France Sorbonne Universités UPMC Université Paris 06 CNRS USR3151 Protein Phosphorylation and Human Disease Unit KISSf Platform Station Biologique Place Georges Teissier Roscoff France

The synthesis of 2-phenylimino-4H-chromene-3-carbonitriles 6(a-d) in good overall yields using an efficient and practical methodology in 3 steps has been implemented in this present work. The first step was a heterocyclization between 2-hydroxybenzaldehyde 1 and propanedinitrile 2 which produced 2-iminocoumarin 3 which was submitted to nitrogen/nitrogen displacement in the presence of aromatic primary amine 4. In the third step, reduction of 5 led to the desired 2-phenylimino-4H-chromene-3-carbonitriles 6. Compounds 5(a-d) and 6(a-d) were evaluated for their potential in vitro cytotoxicity against six selected tumor cell lines (Huh7-D12, Caco2, MDA-MB231, HCT 116, PC3 and NCI-H727) and tested for their protein kinase inhibition on eight selected protein kinases. Among them, compounds 5c and 6b exhibited inhibition on HsCK1e (5c: 44% and 6b: 42% at 1 μM) and 5c for cytotoxicity on PC3 cell lines (63% at 25 μM).

关键词： Iminocoumarin 2H-benzopyran 2-Imino-2H-benzopyran 4H-chromene 2-Amino-4H-chromene Nitrogen/Nitrogen Displacement Protein Kinase Inhibition Cytotoxicity

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欧洲双层列车蓄势待发

国外铁道车辆 2013年第4期50卷 13-14页

作者： Laurent charlier 陈铭

介绍了法国国营铁路公司的TGV 2N2双层列车的结构特点。

关键词：双层列车结构法国

Mineralogy, Petrography and Geochemistry of the Ina Syenite (Linté, Central Cameroon) as a Source of Industrial Feldspars

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Journal of Minerals and Materials Characterization and Engineering 2022年第3期10卷 287-318页

作者： Soualiou Njimbouombouo Mouliom André Njoya Rose Yongue Fouateu Nguo Silvestre Kanouo Daniel Lamilen Mbila Bernard charlier Nathalie Fagel Département de Géologie Université de Liège Liège Belgique Département des Géosciences Université de Yaoundé I Yaoundé Cameroun Mission de Promotion des Matériaux Locaux Yaoundé Cameroun Institut des beaux-arts Université de Dschang Foumban Cameroun Mineral Exploration and Ore Genesis Unit Department of Mining Engineering and Mineral Processing Faculty of Mines and Petroleum Industries University of Maroua Maroua Cameroon

The syenite from Ina (Central region of Cameroon) constitutes a 1000 km2 syntectonic batholith intruded in the Paleoproterozoic granitic basement. The aim of this work is to assess the potential of the Ina batholith syenite as a feldspar minerals resource for industrial use through petrographic and geochemical characterization. Most of the rocks are grey coloured and consist of shimmering feldspar phenocrysts in a fine-grained ferromagnesian matrix. Petrography reveals the presence of two major syenite facies: a widely distributed porphyritic syenite and a less-abundant massive syenite. These facies are dominated by phenocrysts of sub-automorphic perthitic orthoclase. Its malgachite face is due to the presence of numerous inclusions of opaque minerals observed by scanning electron microscopy (ESEM-EDX). Plagioclase phenocrysts have a zonal texture characterised microscopically by an oscillatory compositional zonation. Biotite, hornblende and augite, identified by X-ray powder diffraction, are finely disseminated in the feldspar matrix. Quartz appears as small automorphic crystals with maximum abundance of about 4 wt%. The XRF chemical composition reveals, alongside silica (59.29 wt% to 63.27 wt%), significant proportion of alumina (15.82 wt% to 19.80 wt%), potassium and sodium oxides considered as fluxing elements (K2O + Na2O ≥ 10 wt%). The K2O/Na2O ratio varies between 1.65 and 5.51 (average 2.58). Iron and titanium oxides (1 ≥ wt% Fe2O3 + TiO2 ≥ 5), harmful in ceramic industry, are high as in most other feldspathic sources. The characteristics of the Ina syenite are close to most of the syenite ores used worldwide for ceramics and glass raw materials and necessitates purification and beneficiation treatments. Others rock types have been identified at the study site (granite, monzonite, granodiorite) and are considered as inappropriate as a source of industrial feldspars.

关键词： Ina Syenite Petrography Mineralogy Feldspathic Fluxes

法德联合设计制造的BB475000型货运内燃机车

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国外内燃机车 2008年第1期 5-7页

作者： Laurent charlier[法] 程永陆（译）乔英忍（校）

2004年2月27日法国国营铁路公司与本国的阿尔斯通公司和德国西门子公司签订一份购买500台BB475000型货运内燃机车的合同。文中简要介绍该型机车的主要结构特点、技术参数和法、德两家公司的分工。

关键词：货运内燃机车设计结构技术参数阿尔斯通公司西门子公司