2018

Contribution of the endosomal-lysosomal and proteosomal systems in amyloid-β precursor protein derived fragmants processing.  
Evrard C., Kieulen-Campard P., Coevoet M., Opsomer R., Tasiaux B., Melnyk P., Octave J-N., Buée L., Sergeant N*., Vingtdeux V*.
Front. Cell. Neurosci. 2018, [Accepted].

(Hetero)aryl substituted thaizol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators.  
Rami M., Winum J-Y., Supuran C., Melnyk P., Yous S.
J. Enzyme Inhib. Med. Chem. 2018, [Accepted].

Towards the Discovery of a Novel Class of YAP-TEAD Interaction Inhibitors by Virtual Screening Approach Targeting YAP-TEAD Protein-Protein Interface  
Gibault F., Coevoet M., Sturbaut M., Farce A., Renault N., Allemand F., Guichou J-F., Drucbert A-S., Foulon C., Magnez R., Thuru X., Corvaisier M., Huet G., Chavatte P., Melnyk P., Bailly F*., Cotelle P.
Cancers. 2018, 10, 140-145.

Design and synthesis of 2,6-disubstituted-8-amino imidazo[1,2a]pyridines, a promising privileged structure  
Boulahjar R., Rincon Arias A., Bolteau R., Renault N., Coevoet M., Barczyk A., Duroux R., Yous S., Melnyk P., Agouridas L*.
Bioorg. Med. Chem. 2018, 26, 3296-3307.

New phenylaniline derivatives as modulators of amyloid protein precursor metabolism  
Gay M., Carato P., Coevoet M., Renault N., Larchanché P-E., Barczyk A., Yous S., Buée L., Sergeant N., Melnyk P*.
Bioorg. Med. Chem. 2018, 26, 2151-2164.

Antagonists of the adenosine A(2A) receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5-and C7-positions to enhance affinity  
Duroux R., Agouridas L., Renault N., El Bakali J., Furman C., Melnyk P., Yous S*.
Eur. J. Med. Chem. 2018, 144, 151-163.

A Phenotypic Approach to the Discovery of Compounds that Promote Non-Amyloidogenic Processing of the Amyloid Precursor Protein: Toward a New Profile of Indirect β-Secretase Inhibitors  
Gay M., Evrard C., Descamps F., Carato P., Renault N., Coevoet M., Eddarkaoui S., Baud C., Larchanché P-E., Buée L., El Bakali J*., Vingtdeux V*., Sergeant N., Melnyk P.
Eur. J. Med. Chem. 2018, 159, 104-125.

Targeting Transcriptional Enhanced Associate Domains (TEADs).
Gibault F., Sturbaut M., Bailly F., Melnyk P., Cotelle P.*
J. Med. Chem. 2018, 61 (12), 5057-5072

2017

Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners  
Duroux R., Ciancetta A., Mannes P., Yu J., Boyapati S., Gizewski E., Yous S., Ciruela F., Auchampach J-A., Gao Z-G., Jacobson K-A.*
MedChemComm. 2017 , 8, 1659-1667

Synthesis and Biological Evaluation of new Naphtho- and Quinolinocyclopentane Derivatives as Potent Melatoninergic (MT1/MT2) and Serotoninergic (5-HT2C) Dual Ligands  
Duroux R., Rami M., Landagaray E., Ettaoussi M., Caignard D-H., Delagrange P., Melnyk P., Yous S.*
Eur. J. Med. Chem. 2017, 141 (14), 552-566

Synthesis and pharmacological evaluation of benzamide derivatives as potent and selective sigma-1 ligands 
Donnier-Maréchal M., Carato P., Larchanché P-E., Ravez S., Boulahjar R., Barczyk A, Oxombre B., Vermersch P., Melnyk P.*
Eur. J. Med. Chem. 2017, 138, 964-978.

Anti-diabetic activity of fused PPAR Gama-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression 
Pirat C., Dacquet C., Leclerc V., Hennuyer N., Beucher-Gaudin M., Zanirato G., Géant A., Staels B., Ktorza A., Farce A., Caignard D-H., Berthelot P., Lebegue N.
Eur. J. Med. Chem. 2017, 137, 310-326.

Identifiaction of 2-aryl benzoxazole as promising hit for A2A receptor with improved aqueous solubility 
Duroux R., Renault N., Cuelho Esteves J., Agouridas L., Blum D., Lopes L., Melnyk P., Yous S.
J. Enzyme Inhib. Med. Chem. 2017, 32 (1), 850-864. Download

 

 

Inhibition of hepatitis B virus replication by N-hydroxyisoquinolinediones and related polyoxygenated heterocycles. 
Edwards T-C., Lomonosova E., Patel J-A., Li Q., Villa J-A., Gupta A-K., Morrison L-A., Bailly F., Cotelle P., Giannakopoulou E., Zoidis G., Tavis J-E.
Antiviral Res. 2017, 143, 205-217.

Challenges and Opportunities in the Development of Serine Synthetic Pathway Inhibitors for Cancer Therapy. 
Ravez S., Spillier Q., Marteau R., Feron O., Frédérick R.
J. Med. Chem. 2017, 60 (4), 1227-12.

α-Ketothioamide Derivatives: A Promising Tool to Interrogate Phosphoglycerate Dehydrogenase (PHGDH). 
Ravez S., Corbet C., Spillier Q., Dutu A-D., Mullarky E., Cantley L-C., Feron O., Frédérick R.
J. Med. Chem. 2017, 60 (4), 1591-1597.

New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation 
Landagaray E., Ettaoussi M., Rami M., Boutin J.A., Caignard D-H., Delagrange P., Melnyk P., Berthelot P., Yous S.
Eur. J. Med. Chem. 2017, 127, 621-631.

2016

(5Z)-3-(2-Oxopropyl)-5-(3,4,5-trimethoxybenzyl-idene)-1,3-thiazolidine-2,4-dione 
Mague J.T., Mohamed S. K., Akkurt M., El-Kashef H., Lebegue N., Albayati R. M.
IUCrData. 2016, [accepted].

Synthesis and Biological Evaluation of ABT-751 Tricyclic Analogues as Antimitotic and Antivascular Agents with Potent in Vivo Antitumor Activity. 
Segaoula Z., Leclercq J., Verones V., Flouquet N., Lecoeur M., Ach L., Renault N., Barczyk A., Melnyk P., Berthelot P., Thuru X., Lebegue N.
J. Med. Chem. 2016, 59(18), 8422-40.

Identification of a New Benzimidazole Derivative as an Antiviral against Hepatitis C Virus.
Vausselin T., Lemasson M., Lavie M., Séron K., Belouzard S., Fénéant L., Danneels A., Cocquerel L., Rosenberg A., Melnyk P., Dubuisson J.
J. Virol. 201690(19):8422-34.

Synthesis of triazoloquinazolinone based compounds as tubulin polymerization inhibitors and vascular disrupting agents
Driowya M., Leclercq J., Verones V., Barczyk A., Lecoeur M., Renault N., Flouquet N., Ghinet A., Berthelot P., Lebegue N.
Eur. J. Med. Chem. 2016, 115, 393-405.

2-Hydroxyisoquinoline-1,3(2H, 4H)-diones (HIDs) as Human Immunodeficiency Virus Type 1 Integrase Inhibitors: Influence of the Alkylcarboxamide Substitution of Position 4
Billamboz M., Suchaud V., Bailly F., Lion C., Andréola M-L., Christ F., Debyser Z., Cotelle P.
Eur. J. Med. Chem. 2016, 117, 256–268.

Design of experiments for enantiomeric separation in supercritical fluid chromatography
Landagaray E., Vaccher C., Yous S., Lipka E.
J. Pharm. Biomed. Anal. 2016, 120, 297-305.

Non-photoinduced biological properties of verteporfin.
Gibault F., Corvaisier M., Bailly F., Huet G., Melnyk P., Cotelle P. 
Curr. Med. Chem. 2016, 23(11):1171-84.

Melatonergic Ligands: Design, Synthesis and Pharmacological Evaluation of Novel Series of Naphthofuranic Derivatives
Landagaray E., Ettaoussi M., Duroux R., Boutin J-A., Caignard D-H., Delagrange P., Melnyk P., Berthelot P., Yous S.
Eur. J. Med. Chem. 2016, 109, 360-370.

2015

The preclinical discovery and development of dolutegravir for the treatment of HIV.
Bailly F., Cotelle P.
Exp. Opin. Drug Disc. 2015, 10, 1243-1253.

Synthesis and pharmacological evaluation of benzannulated derivatives as potent and selective sigma-1 protein ligands.
Donnier-Maréchal M., Carato P., Le Broc D., Furman C., Melnyk P.
Eur. J. Med. Chem. 2015, 92, 575-582.

Carboline- and phenothiazine-derivated heterocycles as potent sigma-1 ligands.
Donnier-Maréchal M., Larchanché P-E., Le Broc D., Furman C., Carato P., Melnyk P. 
Eur. J. Med. Chem. 2015, 89, 198-206.

Synthesis and pharmacological evaluation of dual ligands for melatonin (MT1/MT2) and serotonin 5-HT2C receptor subtypes (II).
Ettaoussi M., Peres B., Errazani A., Boutin J-A., Caignard D-H., Delagrange P., Melnyk P., Berthelot P., Yous S.
Eur. J. Med. Chem. 2015, 90, 822-833.

PM6280 and PM6577 : ADME study of two potent and anti-malarial amodiaquine analogs with improved metabolic stability.
Hochart G., Paunescu E., Boll E., Melnyk P.
Research and Reviews : J. Org. Med. Chem. 2015, 2, 1-14.

6-Sulfonylbenzothiazolones as potential scaffolds for the design of 5-HT6 ligands.
Larchanché P-E., Ultré V., Le Broc D., Ballandone C., Furman C., Dallemagne P., Melnyk P., Carato P.
Eur. J. Med. Chem. 2015, 92, 807-817.

Efficient Synthesis of 1,3-Disubstituted-1,3-Dihydro-2H-imidazo[5,1-b]quinazolin-9-ones via an Intramolecular Mannich-Type Reaction.
Leclercq J., Driowya M., Flouquet N., Berthelot P., Lebegue N.
Synthesis.  2015, 47, 377-386.

Chloroquine and chloroquine related compounds as a model for the design of anti-Alzheimer compounds.
Melnyk P., Vingtdeux V., Burlet S., Eddarkaoui S., Grosjean M-E., Larchanché P-E., Hochart G., Sergheraert C., Estrella C., Barrier M., Poix V., Plancq P., Lannoo C., Hamdane M., Delacourte A., Verwaerde P., Buée L., Sergeant N.
ACS Chem. Neurosci. 2015, 6, 559-569. Highlighted in ACS Chemical Research in Toxicology

High-affinity σ1 protein agonist reduces clinical and pathological signs of experimental autoimmune encephalomyelitis
Oxombre B., Lee-Chang C., Duhamel A., Toussaint M., Giroux M., Donnier-Maréchal M., Carato P., Lefranc D., Zephir H., Prin L., Melnyk P., Vermersch P.
Br. J. Pharmacol. 2015, 172, 1769-1782.

Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines.
Moas-Héloire V., Renault N., Batalha V-L., Rincon Arias A., Marchivie M., Deguine N., Buée L., Chavatte P., Yous S., Blum D., Lopez LV., Melnyk P., Agouridas L.
Eur. J. Med. Chem.  2015, 106, 15-25.

Conformational restriction leading to a selective CB2 cannabinoid receptor agonist orally active against colitis.
El Bakali J., Muccioli G.G., Body-Malapel M., Djouina M., Klupsch F., Ghinet A., Barczyk A., Renault N., Chavatte P., Desreumaux P., Lambert D-M., Millet R.
ACS Med. Chem. Lett. 2015, 6, 198–203.

 

Structure–activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme
Charton J., Gauriot M., Totobenazara J., Hennuyer N., Dumont J., Bosc D., Marechal X., El Bakali J., Herledan A., Wen X., Ronco C., Gras-Masse H., Heninot A., Pottiez V., Landry V., Staels B., Liang W., Leroux F., Tang W. J, Deprez B., Deprez-Poulain R.
Eur. J. Med. Chem. 2015, 90, 547–567.

2014

Thiocarbamate-linked polysulfonate-peptide conjugates as selective hepatocyte growth factor receptor binders.
Besret S., Vicogne J., Dhamani F., Fafeur V., Desmet R., Drobecq H., Romieu A., Melnyk P., Melnyk O.
Bioconjugate Chem 2014 , 25: 1000-1010. [Open Access]

Pharmacokinetic Evaluation of a Novel Benzopyridooxathiazepine Derivative as a Potential Anticancer Agent .
Bourdon F., Lecoeur M., Lebegue N., Gressier B., Luyckx M., Odou P., Dine T., Goossens J-F., Kambia N.
Pharmacology 2014, 94: 170-178.

Hepatitis B Virus replication is blocked by a 2-hydroxyisoquinoline-1,3(2H,4H)-dione (HID) inhibitor of the viral ribonuclease H activity.
Cai C-W., Lomonosova E., Moran E-A., Cheng X., Patel K-B., Bailly F., Cotelle P., Meyers M-J, Tavis J-E.
Antivir Res 2014, 108:48-55.

Synthesis, chiral resolution, absolute configuration assignment and pharmacological evaluation of a series of melatoninergic ligands.
Ettaoussi M., Pérès B., Jarry C., Pallage V., Nosjean O., Boutin JA., Gohier A., Mannoury la Cour C., Caignard D-H., Delagrange P., Berthelot P., Yous S.
MedChemComm 2014, 5: 1590-1590.

Recovery of brain biomarkers following PPAR agonist neuroprotective treatment before ischemic stroke.
Gelé P., Vingtdeux V., Drobecq H., Melnyk P., Ghestem A., Buée L., Sergeant N., Bordet R.
Proteome Science 2014, 12: 24.

New Melatonin (MT1/MT2) Ligands: Design and Synthesis of (8,9-Dihydro-7H-furo[3,2-f]chromen-1-yl) Derivatives.
Landagaray E., Ettaoussi M., Leclerc V., Perez V., Nosjean O., Boutin J-A., Caignard D-H., Delagrange P, Berthelot P., Yous S.
Bioorg. Med. Chem.  2014, 22: 986-996.

Enhanced detection for determination of enantiomeric purity of novel agomelatine analogs by EKC using single and dual cyclodextrin systems.
Lipka E., Landagaray E., Ettaoussi M., Yous S., Vaccher C.
Electrophoresis.  2014, 35: 2785-2792.

Phenylthiocarbamate or N-carbothiophenylgroup chemistry in peptide synthesis or bioconjugation
Melnyk O., Ollivier N., Besret S., Melnyk P.
Bioconjugate Chem.  2014 , 25: 629-39. [Open Access]

Targeting A2A receptor to treat neurodegenerative diseases: design, synthesis and evaluation of potential antagonists.
Moas-Héloire V., Renault N., Batalha V-L., Chavatte P., Yous S., Buée L., Blum D., Lopez L-V., Agouridas L., Melnyk P.
Purinergic Signalling.  2014, 10:663-4.

Investigation of a Novel Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as Human Immunodeficiency Virus Type 1 Integrase Inhibitors 

Suchaud V., Bailly F., Lion C., Calmels C., Andréola M-L., Christ F., Debyser Z., Cotelle P.
J. Med. Chem.  2014, 57:4640-4660.

Unexpected Heteroannelation and Chlorination of Benzothiadiazine Derivatives mediated by DDQ.
Verones V., Flouquet N., Farce A., Berthelot P., Lebegue N.
Synthesis.  2014 , 46:235-241.

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.
El Bakali J., Gras-Masse H., Maingot L., Deprez B., Dumont J., Leroux F., Deprez-Poulain R.
Future Med. Chem. 2014, 6: 1381–1397.

NMR studies of interactions of new CB2 cannabinoid receptor ligands with cyclodextrins hosts. Correlation with micellar electrokinetic chromatography and reversed phase high performance liquid chromatography.
Azaroual N., El Bakali J., Le Broc D., Deghaye C., Farce A., Chavatte P., Millet R., Vaccher C., Lipka-Belloli E.
J. Incl. Phenom. Macrocycl. Chem. 2014, 78: 265–274.

2013

Tau pathology modulates Pin1 post-translational modifications and may be relevant as biomarker.
Ando K., Sambo AV., Dourlen P., Bretteville A., Belarbi K., Vingtdeux V., Eddarkaoui S., Drobecq H., Ghestem A., Begard S., Demey-Thomas E., Melnyk P., Smet C., Lippens G., Maurage C-A., Caillet-Boudin M-L., Verdier Y., Vinh J., Landrieux I., Galas M-C., Blum D., Hamdane M., Sergeant N., Buée L.
Neurobiol. Aging. 2013, 34: 757-769.

Antiproliferative and apoptotic effects of the oxidative dimerization product of methyl caffeate on human breast cancer cells.
Bailly F., Toillon R-A., Tomavo O., Jouy N., Hondermarck H., Cotelle P.
Bioorg. Med. Chem. Lett. 2013, 23: 574-578.

4-substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a novel class of HIV-1Integrase inhibitors.
Billamboz M., Suchaud V., Bailly F., Lion C., Demeulemeester J., Calmels C., Andréola M-L., Christ F., Debyser Z., Cotelle P.
ACS Med. Chem. Lett. 2013, 4: 606-611.

In vitro pharmacokinetic profile of a benzopyridooxathiazepine derivative using rat microsomes and hepatocytes: Identification of phases I and II metabolites.
Bourdon F., Lecoeur M., Verones V., Vaccher C., Lebegue N., Dine T., Kambia N., Goossens JF.
J. Pharm. Biomed. Anal. 2013, 80 : 69-78.

2-Hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs), novel inhibitors of HIV integrase with a high barrier to resistance.
Desimmie B-A., Demeulemeester J., Suchaud V., Taltynov O., Billamboz M., Lion C., Bailly F., Strelkov S., Debyser Z., Cotelle P., Christ F.
ACS Chem. Biol. 2013, 8 : 1187-1194.

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 D-H., Delagrange P., Berthelot P., Yous S.
ChemMedChem. 2013 , 8: 1830-1845.

Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches.
Gonzalbez R., Mozulén S., Carbajo R., Melnyk P., Pineda-Lucena A.
Bioorg. Med. Chem. 2013, 21: 1944-1951.

New radioligands for the description of MT1 and MT2 melatonin receptor molecular pharmacology.
Legros C., Matthey U., Grelak T., Pedragosa-Moreau S., Hasseler W., Yous S., Thomas E., Suzenet F., Folleas B., Lefoulon F., Berthelot P., Caignard D-H., Guillaumet G., Delagrange P., Brayer J-L., Nosjean O., Boutin J-A.
Int. J. Mol. Sci. 2013, 14: 8948-8962.

Exploring 6-(substituted sulfonyl)imidazopyridines as a potential scaffold for the design of 5-HT6 ligands.
Moas-Heloire V., Furman C., Melnyk P., Carato P.
Monatsch Chem. 2013 , 144: 425-435.

Synthesis, antiproliferative activity and tubulin targeting effect of acridinone and dioxophenothiazine derivatives.
Verones V., Flouquet N., Lecoeur M., Lemoine A., Farce A., Baldeyrou B., Mahieu C., Wattez N., Lansiaux A., Goossens J-F., Berthelot P., Lebegue N.
Eur. J. Med. Chem 2013, 59: 39-47.

2012

Methodology to Access Tetrahydrodipyridoimidazole Derivatives
Mohamed El Bousmaqui, Marion Donnier-Marechal, Paul-Emmanuel Larchanche, Patricia Melnyk, and Pascal Carato
Heterocycles 2012, 85: 2135-2145.

Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (
Ettaoussi M., Sabaouni A., Rami M., Boutin J-A, Delagrange P., Renard P., Spedding M., Caignard D-H., Berthelot P., Yous S.
Eur. J. Med. Chem. 2012, 49: 310-323.

Stereoselective synthesis of enantiopure N-protected-3-aryl piperazines from keto-esters.
Jida M., Laconde G., Soueidan O-M., Lebegue N., Revelant G., Pelinski L., Agbossou-Niedercorn F., Deprez B., Deprez-Poulain R.
Tetrahedron. Lett 2012, 53: 5215-5218.

Effect of Oxime Ether Incorporation in Acyl Indole Derivatives on PPAR Subtype Selectivity.
Le Naour M., Leclerc V., Farce A., Caignard D-H., Hennuyer N., Staels B., Audinot-Bouchez V., Boutin J-A., Lonchampt M., Dacquet C., Ktorza A., Berthelot P., Lebegue N.
Chem. Med. Chem. 2012 , 7: 2179-2193.

Targeting Peroxisome Proliferator-Activated Receptors (PPARs): Development of Modulators.
Pirat C., Farce A., Lebegue N., Renault N., Furman C., Millet R., Yous S., Speca S., Berthelot P., Desreumaux P., Chavatte P.
J. Med. Chem. 2012, 55: 4027-4061.

Novel Conformationally Constrained Analogues of Agomelatine as New Melatoninergic Ligands.
Rami M., Landagaray E., Ettaoussi M., Boukhalfa K., Caignard D-H., Delagrange P., Berthelot P., Yous S.
Molecules 2012, 18: 154-166.

Development of a series of 3-hydroxyquinolin-2(1H)-ones as inhibitors of HIV-1 reverse transcriptase associated RNase H activity.
Suchaud V., Lion C., Tramontano E., Esposito F., Corona A., Christ F., Debyser Z., Cotelle P.
Bioorg. Med. Chem. Lett 2012 , 22: 3988-3992.

Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation.
El Bakali J., Maingot L., Dumont J., Host H., Hocine A., Cousaert N., Dassonneville S., Leroux F., Deprez B., Deprez-Poulain R.
Med. Chem. Commun. 2012, 3:469–474.

Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles.
Wen X., El Bakali J., Deprez-Poulain R., Deprez B.
Tetrahedron Lett. 2012, 53: 2440–2443.

4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands part 2: discovery of new agonists endowed with protective effect against experimental colitis.
El Bakali J., Gilleron P., Body-Malapel M., Mansouri R., Muccioli G.G., Djouina M., Barczyk A., Klupsch F., Andrzejak V., Lipka E., Furman C., Lambert D-M., Chavatte P., Desreumaux P., Millet, R.
J. Med. Chem. 2012, 55: 8948–8952.