A5088160200- Synthesis and Biological Evaluation
- Catalytic C–H Functionalization Methods
- Synthesis and Characterization of Heterocyclic Compounds
- Lanthanide and Transition Metal Complexes
- Click Chemistry and Applications
- Synthesis and Catalytic Reactions
- Chemical Reaction Mechanisms
- Catalytic Cross-Coupling Reactions
- Chemical Synthesis and Analysis
- Sulfur-Based Synthesis Techniques
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and Reactivity of Heterocycles
- Circadian rhythm and melatonin
- Synthesis and biological activity
- Synthesis and Reactions of Organic Compounds
- Fluorine in Organic Chemistry
- Receptor Mechanisms and Signaling
- Metal complexes synthesis and properties
- Molecular Sensors and Ion Detection
- Synthesis of heterocyclic compounds
- Pharmacological Receptor Mechanisms and Effects
- Phenothiazines and Benzothiazines Synthesis and Activities
- Chemical Synthesis and Reactions
- Luminescence and Fluorescent Materials
Université d'Orléans
2016-2025
Institut de Chimie Organique et Analytique
2015-2024
Centre National de la Recherche Scientifique
2015-2024
Les Hôpitaux de Chartres
2015-2018
California Earthquake Authority
2018
Commissariat à l'Énergie Atomique et aux Énergies Alternatives
2003-2016
Bipar
2015
Université de Rouen Normandie
2015
Peking University
2015
Centre National pour la Recherche Scientifique et Technique (CNRST)
2013
G protein-coupled receptors (GPCRs) are classically characterized as cell-surface transmitting extracellular signals into cells. Here we show that central components of a GPCR signaling system comprised the melatonin type 1 receptor (MT
We report two prototype Ln3+complexes that address requirements for both MRI and luminescence imaging we demonstrate the presence of H2O molecules bound to Ln3+, beneficial applications Gd3+ analogue, is not a major limitation development NIR luminescent agents.
Abstract A series of novel triazole derivative pyridine‐based polyamino–polycarboxylate ligands has been synthesized for lanthanide complexation. This versatile platform chelating agents combines advantageous properties both magnetic resonance (MR) and optical imaging applications the corresponding Gd 3+ near‐infrared luminescent complexes. The thermodynamic stability constants Ln complexes, as assessed by pH potentiometric measurements, are in range log K LnL =17–19, with a high selectivity...
Abstract A hybrid coumarin–thiazole compound was developed as a novel ratiometric and colorimetric sensor for bisulfite anions. Structure identification of the confirmed by 1 H NMR, 13 C H, COSY, heteronuclear single quantum coherence (HSQC), IR, HRMS spectroscopy. The detection anions performed through Michael addition anion toward sensor. reaction between caused fluorescence intensity to decrease at 600 nm increase 450 simultaneously yielded visible color change from purplish red colorless...
[reaction: see text] Palladium-catalyzed cross-coupling of vinyl- and arylstannanes with pi-electron-deficient heteroaromatics was performed in good yields. This Stille-type reaction carried out a methylthioether function as an electrophile the presence copper(I) bromide-dimethyl sulfide complex.
In the objective of developing ligands that simultaneously satisfy requirements for MRI contrast agents and near-infrared emitting optical probes are suitable imaging, three isoquinoline-based polyaminocarboxylate ligands, L1, L2 L3, have been synthesized corresponding Gd3+, Nd3+ Yb3+ complexes investigated. The specific challenge present work was to create NIR which (i) excitation wavelengths compatible with biological applications (ii) able emit a sufficient number photons ensure sensitive...
Background and Purpose The paradigm that GPCRs are able to prolong or initiate cellular signalling through intracellular receptors recently emerged. Melatonin binds G protein‐coupled MT 1 2 receptors. In contrast most other hormones targeting GPCRs, melatonin its synthetic analogues amphiphilic molecules easily penetrating into cells, but the existence of is still unclear mainly due a lack appropriate tools. Experimental Approach We therefore designed synthesized series hydrophilic receptor...
Here, we examine the photophysical properties of five ruthenium(II) complexes comprising two 4,7-diphenyl-1,10-phenanthroline (dip) ligands and functionalized bipyridine (R1bpy-R2, where R1 = H or CH3, R2 H, COO−,4-[3-(2-nitro-1H-imidazol-1-yl)propyl] 1,3-dicyclohexyl-1-carbonyl-urea) towards development luminescence probes for cellular imaging. These have been shown to interact with albumin formed adducts exhibited up eightfold increase in quantum yield as well average lifetime emission. It...
Cyclic thionocarbamates, namely chiral oxazolidinethiones (OZT) and aromatic oxazolinethiones (OXT), were involved, for the first time, in Sonogashira cross-coupling. A cooperative effect of two different copper (I) speciesCuI CuTCaccounts this new copper-catalyzed desulfurative carbon−carbon cross-coupling reaction. This reactivity could also be extended to other catalysts.
In an effort toward the visualization of β-amyloid plaques by in vivo imaging techniques, we have conjugated optimized derivative Pittsburgh compound B (PiB), a well-established marker Aβ plaques, to DO3A-monoamide that is capable forming stable, noncharged complexes with different trivalent metal ions including Gd(3+) for MRI and (111)In(3+) SPECT applications. Proton relaxivity measurements evidenced binding Gd(DO3A-PiB) amyloid peptide Aβ1-40 human serum albumin, resulting two- four-fold...
The α-3-(1,2,4-triazine)-α-cyanoacetate derivatives exhibit a unique and well-defined dearomatized structure undergoing efficient organocatalytic aromatization–alkylation sequences with Michael acceptors in order to construct an all-carbon tetrasubstituted stereocenter high ee values. These new players the field of enantioselective catalytic benzylic C–H functionalization afford versatile molecular platforms toward construction valuable 3D-heterocycles.
The palladium-catalyzed coupling reaction of 3-thiomethyl-1,2,4-triazine 1 with different organoboron compounds in the presence copper(I) 3-methylsalicylate proceeds to afford corresponding 3-substituted-1,2,4-triazines good yield. This approach leads very easily a large range C-5 and C-6 unsubstituted as-triazines.
Contrary to the common idea that Fischer indole cyclization often cannot be effectively applied synthesis of corresponding azaindoles, we show this approach can actually very efficient for formation 4- and 6-azaindoles bearing an electron-donating group on starting pyridylhydrazines. Two 4-azaindole natural product analogues were synthesized in a few steps good overall yields.
Using intramolecular charge transfer (ICT) as a signaling mechanism, series of hybrid coumarin–hemicyanine compounds were synthesized chemosensors for cyanide detection by taking advantage cyanide's strong affinity toward the polarized CN bond hemicyanine group. Structure identification was confirmed 1H NMR, 13C 1H-1H COSY, HSQC, IR, and HRMS spectroscopy. Multiple sensory signals are available can be used both qualitative monitoring quantitative determination cyanide, including...
The studied Ru polypyridyl complexes are<italic>ca.</italic>ten times more cytotoxic against breast cancer (4T1) and human lung adenocarcinoma epithelial cells (A549) than cisplatin have a distinct impact on cell adhesion, migration endothelial vasculature.
The effect of polypyridyl Ru(II) complexes on the ability cancer cells to migrate and invade, two features important in formation metastases, is evaluated. In vitro studies are carried out breast cell lines, MDA-MB-231 MCF-7, as well melanoma lines A2058 A375. Three comprising 4,7-diphenyl-1,10-phenanthroline (dip) ligands a third ligand 2,2′-bipyridine (bpy), or its derivative with either 4-[3-(2-nitro-1H-imidazol-1-yl)propyl] (bpy-NitroIm),...
In the present study, new 2-phenyl-5,6,7,8-tetrahydroimidazo [1,2-
In this paper, N-arylations between two heteroaryl compounds were studied. Conditions found to generate selectively either 3- or 5-heteroarylamino-1,2,4-triazines by investigating anionic processes (use of bases such as 2,2',6,6'-tetramethylpiperidine/tBuOK/nBuLi) Pd-catalyzed [Pd(OAc)(2), xantphos]. These methods successfully applied a wide variety heteroarylamines and allowed us pursue our work on fused polynitrogen synthesis.
A novel method was developed for the preparation of N-fused heterocycles via a Csp–S coupling reaction and sequence 5-endo-dig cyclization. This involves –NHC(S)NH-containing compounds alkynes in presence CuCl N,N′-dicyclohexylimidazolium chloride.
Melatonin receptors have been studied for several decades. The low expression of the in tissues led scientific community to find a substitute natural hormone melatonin, agonist 2-[125I]-iodomelatonin. Using agonist, hundreds studies were conducted, including discovery agonists and antagonists minute details about their molecular behavior. Recently, we attempted expand panel radioligands available studying melatonin by using newly discovered compounds SD6, DIV880, S70254. These characterized...
Abstract A series of novel pyridine‐based Gd 3+ complexes have been prepared and studied as potential MRI contrast agents for Zn 2+ detection. By independent assessment molecular parameters affecting relaxivity, we could interpret the relaxivity changes observed upon binding in terms variations rotational motion.
A straightforward domino aza-Michael-inverse-electron-demand-hetero-Diels–Alder/retro-Diels–Alder reaction between primary and secondary propargylamine derivatives 3-vinyl-1,2,4-triazines is developed highlighting not only the uniqueness of this dual-heterocyclic platform but also a novel unprecedented path to polysubstituted tetrahydro-1,6-naphthyridine scaffolds.