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Items: 1 to 20 of 44


New piperazine multi-effect drugs prevent neurofibrillary degeneration and amyloid deposition, and preserve memory in animal models of Alzheimer's disease.

Sergeant N, Vingtdeux V, Eddarkaoui S, Gay M, Evrard C, Le Fur N, Laurent C, Caillierez R, Obriot H, Larchanché PE, Farce A, Coevoet M, Carato P, Kouach M, Descat A, Dallemagne P, Buée-Scherrer V, Blum D, Hamdane M, Buée L, Melnyk P.

Neurobiol Dis. 2019 Mar 27. pii: S0969-9961(18)30327-9. doi: 10.1016/j.nbd.2019.03.028. [Epub ahead of print]


(Hetero)aryl substituted thiazol-2,4-yl scaffold as human carbonic anhydrase I, II, VII and XIV activators.

Rami M, Winum JY, Supuran CT, Melnyk P, Yous S.

J Enzyme Inhib Med Chem. 2019 Dec;34(1):224-229. doi: 10.1080/14756366.2018.1543292.


Contribution of the Endosomal-Lysosomal and Proteasomal Systems in Amyloid-β Precursor Protein Derived Fragments Processing.

Evrard C, Kienlen-Campard P, Coevoet M, Opsomer R, Tasiaux B, Melnyk P, Octave JN, Buée L, Sergeant N, Vingtdeux V.

Front Cell Neurosci. 2018 Nov 22;12:435. doi: 10.3389/fncel.2018.00435. eCollection 2018.


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 PE, Buée L, El Bakali J, Vingtdeux V, Sergeant N, Melnyk P.

Eur J Med Chem. 2018 Nov 5;159:104-125. doi: 10.1016/j.ejmech.2018.08.092. Epub 2018 Sep 22.


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 Jul 23;26(12):3296-3307. doi: 10.1016/j.bmc.2018.04.057. Epub 2018 Apr 30.


Toward 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 JF, Drucbert AS, Foulon C, Magnez R, Thuru X, Corvaisier M, Huet G, Chavatte P, Melnyk P, Bailly F, Cotelle P.

Cancers (Basel). 2018 May 8;10(5). pii: E140. doi: 10.3390/cancers10050140.


New phenylaniline derivatives as modulators of amyloid protein precursor metabolism.

Gay M, Carato P, Coevoet M, Renault N, Larchanché PE, Barczyk A, Yous S, Buée L, Sergeant N, Melnyk P.

Bioorg Med Chem. 2018 May 1;26(8):2151-2164. doi: 10.1016/j.bmc.2018.03.016. Epub 2018 Mar 12.


Antagonists of the adenosine A2A 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 Jan 20;144:151-163. doi: 10.1016/j.ejmech.2017.12.007. Epub 2017 Dec 5.


Targeting Transcriptional Enhanced Associate Domains (TEADs).

Gibault F, Sturbaut M, Bailly F, Melnyk P, Cotelle P.

J Med Chem. 2018 Jun 28;61(12):5057-5072. doi: 10.1021/acs.jmedchem.7b00879. Epub 2017 Dec 28.


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 DH, Delagrange P, Melnyk P, Yous S.

Eur J Med Chem. 2017 Dec 1;141:552-566. doi: 10.1016/j.ejmech.2017.10.025. Epub 2017 Oct 12.


Synthesis and pharmacological evaluation of benzamide derivatives as potent and selective sigma-1 protein ligands.

Donnier-Maréchal M, Carato P, Larchanché PE, Ravez S, Boulahjar R, Barczyk A, Oxombre B, Vermersch P, Melnyk P.

Eur J Med Chem. 2017 Sep 29;138:964-978. doi: 10.1016/j.ejmech.2017.07.014. Epub 2017 Jul 12.


Design, synthesis and evaluation of 2-aryl benzoxazoles as promising hit for the A2A receptor.

Duroux R, Renault N, Cuelho JE, Agouridas L, Blum D, Lopes LV, Melnyk P, Yous S.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):850-864. doi: 10.1080/14756366.2017.1334648.


Molecular Features of the YAP Inhibitor Verteporfin: Synthesis of Hexasubstituted Dipyrrins as Potential Inhibitors of YAP/TAZ, the Downstream Effectors of the Hippo Pathway.

Gibault F, Bailly F, Corvaisier M, Coevoet M, Huet G, Melnyk P, Cotelle P.

ChemMedChem. 2017 Jun 21;12(12):954-961. doi: 10.1002/cmdc.201700063. Epub 2017 Apr 20.


New quinolinic derivatives as melatonergic ligands: Synthesis and pharmacological evaluation.

Landagaray E, Ettaoussi M, Rami M, Boutin JA, Caignard DH, Delagrange P, Melnyk P, Berthelot P, Yous S.

Eur J Med Chem. 2017 Feb 15;127:621-631. doi: 10.1016/j.ejmech.2016.12.013. Epub 2017 Jan 3.


Synthesis and Biological Evaluation of N-[2-(4-Hydroxyphenylamino)-pyridin-3-yl]-4-methoxy-benzenesulfonamide (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 Sep 22;59(18):8422-40. doi: 10.1021/acs.jmedchem.6b00847. Epub 2016 Aug 30.


Identification of a New Benzimidazole Derivative as an Antiviral against Hepatitis C Virus.

Vausselin T, Séron K, Lavie M, Mesalam AA, Lemasson M, Belouzard S, Fénéant L, Danneels A, Rouillé Y, Cocquerel L, Foquet L, Rosenberg AR, Wychowski C, Meuleman P, Melnyk P, Dubuisson J.

J Virol. 2016 Sep 12;90(19):8422-34. doi: 10.1128/JVI.00404-16. Print 2016 Oct 1.


Evaluation of three neutral capillary coatings for the determination of analyte-cyclodextrin binding constants by affinity capillary electrophoresis. Application to N,N'-disubstituted piperazine derivatives.

Danel C, Melnyk P, Azaroual N, Larchanché PE, Goossens JF, Vaccher C.

J Chromatogr A. 2016 Jul 15;1455:163-171. doi: 10.1016/j.chroma.2016.05.090. Epub 2016 May 26.


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. Review.


Melatonergic ligands: Design, synthesis and pharmacological evaluation of novel series of naphthofuranic derivatives.

Landagaray E, Ettaoussi M, Duroux R, Boutin JA, Caignard DH, Delagrange P, Melnyk P, Berthelot P, Yous S.

Eur J Med Chem. 2016 Feb 15;109:360-70. doi: 10.1016/j.ejmech.2015.12.047. Epub 2015 Dec 29.


Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines.

Moas-Héloire V, Renault N, Batalha V, Arias AR, Marchivie M, Yous S, Deguine N, Buée L, Chavatte P, Blum D, Lopes L, Melnyk P, Agouridas L.

Eur J Med Chem. 2015 Dec 1;106:15-25. doi: 10.1016/j.ejmech.2015.10.030. Epub 2015 Oct 19.

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