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Collaborations nationales
* Laboratoire Immunologie, EA2096, LIRIC, CHR Lille (Pr Patrick VERMEERSH)
* EA 1046, CHR Lille (Pr Régis BORDET)
* CIIL, Inserm U1019, CNRS UMR8204, Lille (Dr Jean DUBUISSON)
* CNRS UMR 8576, Lille (Dr Guy LIPPENS)
* Inserm U1053 Bordeaux (Dr Eric CHEVET)
* FRE CNRS 3396 Bordeaux (Pr Christian JARRY)
* Inserm U710 Montpellier (Dr Tangui MAURICE)
* Inserm U692, Université Strasbourg (Dr Luc DUPUIS)
* CNRS UMR 7272, Nice (Dr Nadine MARTINET)
* CNRS UMR 7257, Marseille (Dr Karine ALVAREZ)
* CNRS UMR 5234, Bordeaux (Dr Marie-Line ANDREOLA)

 

 

Collaborations internationales
* Faculté de Chimie, Université de Cluj-Napoca, Roumanie (Pr Ion GROSU)
* Centro de Investigation Principe Felipe, Valencia, Espagne (Dr Antonio PINEDA-LUCENA)
* Universidad de Alicante, Espagne (Pr Nicolas CUENCA)
* Instituto Pluridisciplinar Universidad Complutense, Madrid, Espagne (Pr Aurelio G CSAKY, Pr Sagrario M ARAGON)
* University of Gottingen, Allemagne (Pr Tiago OUTEIRO)
* Instituto de Medicina Molecular, Lisbonne, Portugal (Dr Luisa LOPES)
* Université de Gent, Belgique (Dr Philip MEULEMAN)
* Laboratory for Molecular Virology and Gene Therapy, KU Leuven, Belgique (Pr Zeger DEBYSER)
* Department of Life and Environmental Sciences, Université de Cagliari, Italie (Pr Enzo TRAMONTANO)
* UCL School of Pharmacy, London, UK (Pr Frank KOZIELSKI)

* Assiut University (Egypte, Pr Hussein EL-KHASHEF)
* NIDA Baltimore, USA (Dr Tsung Ping Su)
* Université de St Louis, Missouri, USA (Pr John TAVIS)
* Université de Toledo, Ohio, USA (Dr Don RONNING)

 

 

Collaboration industrielle
* AlzProtect

 

 

 

 

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Hepatitis B Virus replication is blocked by a 2-hydroxyisoquinoline-1,3(2H,4H)-dione (HID) inhibitor of the viral ribonuclease H activity.
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New Melatonin (MT1/MT2) Ligands: Design and Synthesis of (8,9-Dihydro-7H-furo[3,2-f]chromen-1-yl) Derivatives.
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Bioorg Med Chem 2014 22: 986-996.

Enantioseparation and thermodynamic study of naphthalene derivatives, new melatoninergic agonists, on coated amylose [tris(S)-1-phenylethylcarbamate] stationary phase. Transposition to preparative scale.
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Biomedical Chromatography 2014 DOI: 10.1002/bmc.3332

Enhanced detection for determination of enantiomeric purity of novel agomelatine analogs by EKC using single and dual cyclodextrin systems.
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Electrophoresis 2014 35: 2785-2792.

Phenylthiocarbamate or N-carbothiophenylgroup chemistry in peptide synthesis or bioconjugation
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Bioconjugate Chem. 2014 25(4): 629-39.

Compounds, pharmaceutical composition and their use in treating neurodegenerative diseases.
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Brevet européen déposé le 16 juin 2014 sous le n° EP14305919.4.

Beta and gamma-carbolines derivatives for the treatment of neurodegenerative diseases.
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Demande PCT déposée le 27 juin 2014 sous le n° PCT/EP2014/063771.

Investigation of a Novel Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as Human Immunodeficiency Virus Type 1 Integrase Inhibitors
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Unexpected Heteroannelation and Chlorination of Benzothiadiazine Derivatives mediated by DDQ.
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Tau pathology modulates Pin1 post-translational modifications and may be relevant as biomarker.
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Neurobiol Aging 2013 34 (3): 757-769. DOI: 10.1086/669517.

Antiproliferative and apoptotic effects of the oxidative dimerization product of methyl caffeate on human breast cancer cells.
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Bioorg Med Chem. Lett 2013 23: 574-578. DOI: 10.1016/j.bmcl.2012.11.009

4-substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a novel class of HIV-1Integrase inhibitors
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ACS Med Chem Lett. 2013, DOI: 10.1021/ml400009t.

In vitro pharmacokinetic profile of a benzopyridooxathiazepine derivative using rat microsomes and hepatocytes: Identification of phases I and II metabolites.
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2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs), novel inhibitors of HIV integrase with a high barrier to resistance.
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ACS Chem Biol. 2013 DOI: 10.1021/cb4000426.

Synthesis and Pharmacological Evaluation of a series of the Agomelatine Analogues as Melatonin MT1/MT2 Agonist and 5-HT2C Antagonist.
Ettaoussi M, Sabaouni A, Pérès B, Landagaray E, Nosjean O, Boutin JA, Caignard DH, Delagrange P, Berthelot P, Yous S.
Chem Med Chem. 2013 8: 1830-1845.

Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches.
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Bioorg Med Chem. 2013 21: 1944-1951. DOI: 10.1016/j.bmc.2013.01.033.

New radioligands for the description of MT1 and MT2 melatonin receptor molecular pharmacology.
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Exploring 6-(substituted sulfonyl)imidazopyridines as a potential scaffold for the design of 5-HT6 ligands.
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Monatsch Chem. 2013 144(3): 425-435. DOI 10.1007/s00706-012-0893-3.

Synthesis, antiproliferative activity and tubulin targeting effect of acridinone and dioxophenothiazine derivatives.
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γ-carbolines derivatives for the treatment of neurodegenerative diseases.
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β -carbolines derivatives for the treatment of neurodegenerative diseases
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Na-substituted carbolines derivatives for the treatment of neurodegenerative diseases.
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Methodology to access to dihydrodipyridoimidazole.
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Heterocycles 2012 085 (9): 2135-2145. DOI: 10.3987/COM-12-12447.

Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I)
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Stereoselective synthesis of enantiopure N-protected-3-aryl piperazines from keto-esters.
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Structural elucidation of degradation products of a benzopyridooxathiazepine under stress conditions using electrospray orbitrap mass spectrometry – Study of degradation kinetic.
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Effect of Oxime Ether Incorporation in Acyl Indole Derivatives on PPAR Subtype Selectivity.
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Analytical and Preparative Chiral Separation of beta-Carboline Derivatives, LDL Oxidation Inhibitors, Using HPLC and CE Methodologies: Determination of Enantiomeric Purity.
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Targeting Peroxisome Proliferator-Activated Receptors (PPARs): Development of Modulators.
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Novel Conformationally Constrained Analogues of Agomelatine as New Melatoninergic Ligands.
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Development of a series of 3-hydroxyquinolin-2(1H)-ones as inhibitors of HIV-1 reverse transcriptase associated RNase H activity.
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Sulfate salts of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[d] imidazol-2-amine, preparation thereof and use of the same
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2-hydroxyisoquinoline-1,3(2h,4h)-diones and related compounds useful as HIV replication inhibitors
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Composés de type spiroisoxazoline ayant une activité potentialisatrice de l’activité d’un antibiotique-composition et produits pharmaceutiques comprenant de tels composés.
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Kinetics and mechanism of racemisation of Tic-Hydantoins, potent sigma-1 agonists.
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2-Hydroxyisoquinoline-1,3(2H,4H)-diones as inhibitors of HIV-1 integrase and reverse transcriptase RNase H domain: influence of the alkylation of position 4.
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Magnesium chelating 2-hydroxyisoquinoline-1,3(2H,4H)-diones, as inhibitors of HIV-1 integrase and/or the HIV-1 reverse transcriptase ribonuclease H domain: discovery of a novel selective inhibitor of the ribonuclease H function.
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3-Hydroxy-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-ones as new HIV-1 integrase inhibitors WO2011046873 A1.
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Oleuropein and derivatives from olives as Tau aggregation inhibitors.
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A novel and efficient one-pot synthesis of (aminophenyl)carbamic acid esters.
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Antioxydant activity of beta-carboline derivatives in the LDL oxidation model.
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Interactions of bexarotene (LGD1069, Targretin) with the coagulation system.
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Cancer Chemoth Pharm. 2011 201168: 847-54. DOI: 10.1007/s00280-010-1553-0.

Design and synthesis of naphthalenic derivatives as new ligands at the melatonin binding site MT3.
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Step for the Synthesis of Metabolically More Stable Analogs of Amodiaquine.
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Preparation and Pharmacological Evaluation of A Novel Series of 2-(phenylthio) benzo[b]thiophenes As Selective MT2 Receptor Ligands.
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Eur J Med Chem. 2011 46: 1835-1840. DOI: 10.1016/j.ejmech.2011.02.044.

Substituted 1,3-Benzothiazol-2(3H)-ones and Their N-Methyl Analogues by a Palladium Coupling Reaction.
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Separation of Tic-hydantoin enantiomers, potent sigma-1 agonist, by high performance liquid chromatography and capillary electrophoresis.
Cabordery A-C, Toussaint M, Bonte J-P, Melnyk P, Vaccher C, Foulon C.
J Chrom. 2010 A 1217 (24): 3871-5. DOI: 10.1016/j.chroma.2010.04.009.

Old and New Inhibitors of Quinone Reductase 2.
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Chem Biol Interact. 2010 186 (2): 103-109. DOI: 10.1016/j.cbi.2010.04.006.

Efficient microwave-assisted two-step procedure for the synthesis of 1,3-disubstituted-imidazo[1,5-a]quinazolin-5-(4H)-ones.
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Tetrahedron 2010 66: 128-133. DOI: 10.1016/j.tet.2009.11.025.

Optimized synthesis of potent anti-malarial aminoquinoline compounds: More convergent and easy access to analogs.
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Heterocyclic Comm. 2011 16 (4-6): 235.239. DOI: 10.1515/HC.2010.011.

Evaluation of aldose reductase inhibition and docking studies of 6′-nitro and 6′,6”-dinitrorosmarinic acids.
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Dual cyclodextrin system in capillary electrophoresis for direct separation of the four stereoisomers of agonist and antagonist melatoninergic ligands.
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New 2-arylnaphthalenediols and triol inhibitors of HIV-1 integrase – Discovery of a new polyhydroxylated antiviral agent.
Maurin C, Lion C, Bailly F, Touati N, Vezin H, Mbemba G, Mouscadet J-F, Debyser Z, Witvrouw M, Cotelle P (2010)
Bioorg Med Chem. 2010 18: 5194-5201.DOI: 10.1016/j.bmc.2010.05.059.

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands.
Mésangeau C, Pérès B, Descamps-François C, Chavatte P, Audinot V, Coumailleu S, Boutin JA, Delagrange P, Caignard DH, Bennejean C, Renard P, Lesieur D, Berthelot P, Yous S.
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New synthesis of Tic-hydantoins sigma-1 ligands and pharmacological characterization on cocaine-induced stimulant effects.
Toussaint M, Debreu-Fontaine M-A, Maurice T, Melnyk P.
Med Chem. 2010 6(6): 355-73. DOI: 10.2174/157340610793563956.

Sigma-1 ligands : Tic-Hydantoin as a key pharmacophore.
Toussaint M, Mousset D, Foulon C, Jacquemard U, Vaccher C, Melnyk P.
Eur J Med Chem. 2010 45 (1): 256-263. DOI: 10.1016/j.ejmech.2009.10.004.

Synthesis, biological evaluation and docking studies of 4-amino-tetrahydroquinazolino [3,2-e]purine derivatives.
Verones V, Flouquet N, Farce A, Carato P, Leonce S, Pfeiffer B, Berthelot P, Lebegue N.
Eur J Med Chem. 2010 45(12): 5678-5684. DOI:10.1016/j.ejmech.2010.09.022.

Formulation and characterization of polyphenol-loaded lipid nanocapsules.
Barras A, Mezzetti A, Richard A, Lazzaroni S, Roux S, Melnyk P, Betbeder D, Dupont N.
Int J Pharm. 2009 379 (2): 270-277. DOI: 10.1016/j.ijpharm.2009.05.054.

The Facile Synthesis of 4-Alkoxycarbonylisoquinoline-1,3-diones and 5-Alkoxycarbonyl-2-benzazepine-1,3-diones via a Mild Alkaline Cyclization.
Billamboz M, Bailly F, Cotelle P.
J Heterocyclic Chem. 2009 46: 392-398. DOI: 10.1002/jhet.52.

Online H/D exchange liquid chromatography as a support for the mass spectrometric identification of the oxidation products of melatonin.
Collin F, Bonnefont-Rousselot D, Yous S, Marchetti C, Jore D, Gardès-Albert M.
J Mass Spectrom. 2009 44: 318-329. DOI: 10.1002/jms.1508.

New hexahydrodiazocinonaphthyridine triones as HIV-1 integrase inhibitors Merck: WO2008048538 A1.
Cotelle P.
Exp Opinion Therapeut Patents 2009 19: 87-93. DOI:10.1517/13543770802603577.

Synthesis of novel compounds with potential topoisomerase I inhibitors.
Delot M, Carato P, Furman C, Lemoine A, Lebegue N, Berthelot P, Yous S.
Synthesis 2009 22 : 3819-3822. DOI: 10.1055/s-0029-1217007.

Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
Durieux S, Chanu A, Bochu C, Audinot V, Coumailleau S, Boutin J-A, Delagrange P, Caignard D-H, Bennejean C, Renard P, Lesieur D, Berthelot P, Yous S.
Bioorg Med Chem. 2009 17: 2963-2974. DOI: 10.1016/j.bmc.2009.03.023.

Benzopyridooxathiazepine derivatives as novel potent antimitotic agents.
Gallet S, Flouquet N, Carato P, Pfeiffer B, Renard P, Leonce S, Pierre A, Berthelot P, Lebegue N.
Bioorg Med Chem. 2009 17: 1132-1138. DOI: 10.1016/j.bmc.2008.12.039.

Rexinoid Bexarotene Modulates Triglyceride but not Cholesterol Metabolism via Gene-Specific Permissivity of the RXR/LXR Heterodimer in the Liver.
Lalloyer F, Pederson TA, Gross B, Lestavel S, Yous S, Vallez E, Gustafsson JA, Mandrup S, Fiévet C, Staels B, Tailleux A.
Arterioscl Throm Vas. 2009 29, 1488-1495. DOI: 10.1161/ATVBAHA.109.189506.

Replacement of 4’-hydroxy group of Amodiaquine and Amopyroquine by aromatic and aliphatic substituants: Synthesis and Antimalarial Activity.
Paunescu E, Susplugas S, Boll E, Varga R, Mouray E, Grosu I, Grellier P, Melnyk P.
Chem Med Chem. 2009 4 (4) : 549-561. DOI: 10.1002/cmdc.200800318.

S26948, a new specific peroxisome proliferator activated receptor gamma modulator improved in vivo hepatic insulin sensitivity in 48 h lipid infused rats.
Sohn K-AK, Cruciani-Guglielmacci C, Kassis N, Clément L, Ouali F, Caüzac M, Lebegue N, Berthelot P, Caignard D-H, Pégorier J-P, Renard P, Dacquet C, Ktorza A, Magnan C.
Eur J Pharmacol. 2009 608 : 104-111. DOI: 10.1016/j.ejphar.2009.02.033.

Tic hydantoin sigma-1 agonist: pharmacological characterization on cocaine-induced stimulant and appetitive effects.
Toussaint M, Delair B, Foulon C, Lempereur N, Vaccher C, Maurice T, Melnyk P.
Eur Neuropsychopharmacol. 2009 19 : 504-515. DOI:10.1016/j.euroneuro.2009.01.008.

Antioxidant activity of benzoxazolinonic and benzothiazolinonic derivatives in the LDL oxidation model.
Yekini I, Hammoudi F, Martin-Nizard F, Yous S, Lebegue N, Berthelot P, Carato P.
Bioorg Med Chem. 2009 17: 7823-7830. DOI : 10.1016/j.bmc.2009.09.016.

New Heterocycle compounds and uses thereof for the prevention or treatment of diseases involving formation of amyloid plaques and/or where a dysfunction of the APP metabolism occurs.
Melnyk P, Burlet S, Le Fur N, Delacourte A.
Licence accordée à AlzProtect (EP 09 306242.0)

 
L’objectif de notre équipe consiste à concevoir et synthétiser de petites molécules à visée thérapeutique pour le traitement des maladies neurodégénératives et du cancer. Il ne s’agit pas tant de développer des molécules actives mais des candidats médicaments et des outils ou sondes chimiques permettant d’aller explorer des mécanismes biologiques. Ces composés sont conçus rationnellement en utilisant la modélisation moléculaire et l’expertise en chimie médicinale de l’équipe. La phase d’optimisation suit le schéma ci-dessous.

 

image

 

Forte d’une longue expertise en chimie organique et thérapeutique, notre équipe travaille en collaboration étroite avec des physiciens, pharmacologues, biologistes et cliniciens. Nos efforts ont permis de découvrir un médicament, aujourd’hui sur le marché (Agomelatine, Valdoxan®, antidépresseur ligand des récepteurs mélatoninergiques commercialisé par les laboratoires Servier) et un candidat médicament actuellement en phase I des essais cliniques pour le traitement de la maladie d’Alzheimer.
Nos projets actuels se focalisent sur :
1) l’étude et la validation d’une cible biologique novatrice impliquée dans la dégradation des protéines altérées pour le traitement des maladies neurodégénératives via la conception de sondes chimiques pour l’étude du mécanisme et de ligands permettant d’interagir avec cette cible,
2) le développement d’antagonistes du récepteur à l’adénosine A2a impliqué dans les maladies de Parkinson et d’Alzheimer
3) l’étude de plusieurs interactions protéine-protéine, importantes dans le traitement des cancers et la conception de petites molécules organiques susceptibles d’empêcher la formation de ces complexes protéiques.

organigramme EQ PM - juin2016

Equipe PM

 

L’équipe “Onco and Neurochemistry” est issue de la fusion de deux groupes de chimistes organiciens et médicinaux de l’Université Lille 2 (EA4481) et de l’Université Lille 1 (EA4478). Elle est composée de 8 professeurs et maitres de conférences, 3 personnels techniques, des doctorants et post doctorants.
Notre laboratoire se situe à la Faculté des Sciences Pharmaceutiques et Biologiques. Nous bénéficions d’un matériel analytique de pointe et des plateaux techniques de la faculté (RMN, LC-MS, ADME,…).

 


Visite du laboratoire:
  https://www.youtube.com/watch?v=Jx0TBKpCJ0c

 

 

 

 

organigramme EQ MCCH- juin2016

 

 

organigramme EQ BQ - juin2016

 

organigramme EQ VP - juin2016

 

organigramme EQ IVS - juin2016