A5083166178- X-ray Diffraction in Crystallography
- Dendrimers and Hyperbranched Polymers
- Organophosphorus compounds synthesis
- Crystallization and Solubility Studies
- Sulfur-Based Synthesis Techniques
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Chemical Synthesis and Analysis
- Medical Imaging Techniques and Applications
- RNA Interference and Gene Delivery
- Ferrocene Chemistry and Applications
- Radiopharmaceutical Chemistry and Applications
- Cancer, Hypoxia, and Metabolism
- Gastroesophageal reflux and treatments
- Immune Cell Function and Interaction
- Esophageal and GI Pathology
- Click Chemistry and Applications
- Advanced biosensing and bioanalysis techniques
- Immunotherapy and Immune Responses
- Diverticular Disease and Complications
- Neuroendocrine Tumor Research Advances
- Crystallography and molecular interactions
- Glioma Diagnosis and Treatment
- Synthesis of heterocyclic compounds
- Carbohydrate Chemistry and Synthesis
- Synthesis and characterization of novel inorganic/organometallic compounds
Centre National de la Recherche Scientifique
2006-2024
Institut Pluridisciplinaire Hubert Curien
2014-2024
Université de Strasbourg
2016-2024
Université de Caen Normandie
2010-2019
Nutrition, Obésité et Risque Thrombotique
2017
Inserm
2017
NorthShore University HealthSystem
2014
Northwestern University
2014
University of Chicago
2014
Nuvisan (Germany)
2014
Purpose Induction chemotherapy (IC) before radiotherapy lowers distant failure (DF) rates in locally advanced squamous cell carcinoma of the head and neck (SCCHN). The goal this phase III trial was to determine whether IC chemoradiotherapy (CRT) further improves survival compared with CRT alone patients N2 or N3 disease. Patients Methods Treatment-naive nonmetastatic SCCHN were randomly assigned (CRT arm; docetaxel, fluorouracil, hydroxyurea plus 0.15 Gy twice per day every other week)...
Non-natural born killers: The addition of phosphorus-containing dendrimers capped with phosphonate end groups to cultures human peripheral blood mononuclear cells (white cells) strongly stimulates the selective multiplication functional natural killer (NK) (see picture), which play a key role in anticancer immunity. Both generation dendrimer and type are important criteria for activity. Supporting information this article is available on WWW under...
As first defensive line, monocytes are a pivotal cell population of innate immunity. Monocyte activation can be relevant to range immune conditions and responses. Here we present new insights into the by series phosphonic acid-terminated, phosphorus-containing dendrimers. Various dendritic or subdendritic structures were synthesized tested, revealing basic structural requirements for monocyte activation. We showed that multivalent character acid capping dendrimers crucial targeting Confocal...
A first generation phosphorus-containing dendrimer with twelve terminal benzyl dithiobenzoate functions was designed and subsequently used as a multifunctional agent to derive hybrid star copolymers consisting of dendritic core surrounded by polystyrene branches reversible addition-fragmentation chain transfer (RAFT).
An operationally simple and concise synthesis of anilinoethanolamines, as NMDA NR2B receptor antagonist ifenprodil analogues, was developed via a copper-catalyzed amination the corresponding bromoarene. Coupling achieved with linear primary alkylamines, alpha,omega-diamines, hexanolamine benzophenone imine, well aqueous ammonia, in good yields using CuI N,N-diethylsalicylamide, 2,4-pentadione or 2-acetylcyclohexanone catalytic systems. Amination ethylene diamine efficient even absence an...
Fluorescent probes are commonly used in studying G protein-coupled receptors living cells; however their application to the whole animal receptor imaging is still challenging. To address this problem, we report design and synthesis of first near-infrared emitting fluorogenic dimer with environment-sensitive folding. Due formation non-fluorescent H-aggregates an aqueous medium, displays a strong turn-on response (up 140-fold) apolar environment exceptional brightness: 56% quantum yield ≈444...
Despite numerous molecular targeted therapies tested in glioblastoma (GBM), no significant progress patient survival has been achieved the last 20 years overall population of GBM patients except with TTfield setup associated standard care chemoradiotherapy. Therapy resistance is target expression heterogeneity and plasticity between tumors tumor niches. We focused on α5 integrin implicated aggressive preclinical clinical samples. To address characteristics we started data indicating that...
We describe the synthesis and pharmacological characterization of a first generation ifenprodil conjugates 4–7 as fluorescent probes for confocal microscopy imaging NR2B-containing NMDA receptor. The fluorescein conjugate 6 displayed moderate affinity NMDAR but high selectivity NR2B subunit its NTD. Fluorescence DS-red labeled cortical neurons showed an exact colocalization probe with small protrusions along dendrites related to specific binding on NMDARs.
As evidenced by the number of publications and patents published in last years, radiosynthesis 6‐[ 18 F]fluoro‐3,4‐dihydroxy‐ L ‐phenylalanine ([ F]FDOPA) using nucleophilic [ F]F‐ process remains currently a challenge for radiochemists scientific community even if promising methods radiofluorination electron‐rich aromatic structures were recently developed from arylboronate, arylstannane or iodonium salt precursors. In such context, based on use an triflate precursor, we optimized fast...
An efficient method to incorporate the fluorine-18 radionuclide in 2-nitropurine-based nucleosides was developed. The nucleophilic radiofluorination of labeling precursor with [(18)F]KF under aminopolyether-mediated conditions (Kryptofix 2.2.2/K2CO3) followed by deprotection straightforward and, after formulation, gave 2-[(18)F]fluoroadenosine, ready for injection a radiochemical yield 45 ± 5%, purity >98%, and specific radioactivity up 148 GBq/μmol. A micropositron emission tomography...
N-(2-Hydroxyalkyl)-2-phosphonoethanethioamides were prepared from a readily accessible phosphonodithioacetate and commercial chiral β-amino alcohols. Taking advantage of both the presence hydroxy group (nucleofuge) C=S (nucleophile) in same molecule, we obtained new phosphonylated thiazolines by an intramolecular cyclisation using Mitsunobu procedure. These thiazoline-phosphonates then involved Horner-Wadsworth-Emmons reaction to give asymmetric vinylic thiazolines.
The synthesis and characterization of a series five new diaminodithiophosphoric acid esters (R1R2N)2P(S)SR aminotrithiophosphoric (R1R2N)P(S)(SR)2 are described. structure two these compounds, the diaminodithio derivative (iPr2N)2P(S)SCH2Ph aminotrithio (iPr2N)P(S)(SCH2Ph)2, has been determined by single crystal X-ray diffraction. These compounds potentially usable as agents for reversible addition-fragmentation chain transfer polymerization.
[2,3]-sigmatropic rearrangement - diazomethylphosphonate carbene allylic sulfide phosphoryl
Nichtnatürlich geborene Killer: Die Zugabe von phosphorhaltigen Dendrimeren mit Phosphonat-Endgruppen zu Kulturen menschlicher peripherer mononukleärer Blutzellen (weiße Blutzellen) regt die selektive Vermehrung funktioneller natürlicher Killer(NK)-Zellen stark an (siehe Bild), eine Schlüsselrolle bei der Immunität gegen Krebs spielen. Sowohl Erzeugung des Dendrimers als auch Art Endgruppen sind wichtige Kriterien für Aktivität.
Patient premedication with carbidopa seems to improve the accuracy of 6-18F-fluoro-3,4-dihydroxy-l-phenylalanine (18F-FDOPA) PET for insulinoma diagnosis. However, risk false-negative results in presence is a concern. Consequently, we aimed evaluate effect on 18F-FDOPA uptake β-cells and an xenograft model mice.18F-FDOPA vitro accumulation was assessed murine β-cell line RIN-m5F. In vivo small-animal experiments were performed tumor-bearing nude mice after subcutaneous injection RIN-m5F...
The HDA reaction of dithioesters was developed as a new click-reaction compatible with the indirect 18F-labelling peptides. It involves dithioester-peptides and radiofluorinated diene novel prosthetic group. method applied to PSMA-ligand for in vivo detection LNCap tumors xenografted mice.
Diastereoselectivity of up to 88% was achieved for the synthesis an α-mercapto γ-unsaturated phosphonate using readily available chiral dimenthylphosphonyl ester group and a carbanionic [2,3]-sigmatropic rearrangement. Absolute configuration newly formed center this nonracemic thiol determined, corresponding phosphono thiolane S-oxide were also stereoselectively prepared.