P. Melnyk

发表

Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches.

A. Pineda-Lucena, R. Gozalbes, R. Carbajo, 2013, Bioorganic & medicinal chemistry.

Toward the Design of Ligands Selective for the C-Terminal Domain of TEADs.

F. Allemand, M. Gelin, J. Guichou, 2022, Journal of medicinal chemistry.

Discovery of a cryptic site at the interface 2 of TEAD - Towards a new family of YAP/TAZ-TEAD inhibitors.

X. Thuru, F. Bailly, F. Allemand, 2021, European journal of medicinal chemistry.

Toward the Discovery of a Novel Class of YAP–TEAD Interaction Inhibitors by Virtual Screening Approach Targeting YAP–TEAD Protein–Protein Interface

G. Huet, X. Thuru, P. Chavatte, 2018, Cancers.

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

G. Huet, F. Bailly, P. Melnyk, 2017, ChemMedChem.

Parallel synthesis of polysubstituted tetrahydroquinolines

A. Tartar, B. Déprez, P. Melnyk, 1998 .

Sigma-1 ligands: Tic-hydantoin as a key pharmacophore.

C. Foulon, C. Vaccher, P. Melnyk, 2010, European journal of medicinal chemistry.

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

J. Dubuisson, C. Wychowski, A. Mesalam, 2016, Journal of Virology.

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

S. Yous, P. Melnyk, N. Renault, 2017, Journal of enzyme inhibition and medicinal chemistry.

Synthesis of a novel series of (Z)-3,5-disubstituted thiazolidine-2,4-diones as promising anti-breast cancer agents.

Gamal Badr, P. Melnyk, H. El-Kashef, 2020, Bioorganic chemistry.

Direct and Regioselective C(sp3)–H Bond Fluorination of 2-Alkylazaarenes with Selectfluor

P. Melnyk, C. Rolando, M. Penhoat, 2020, Synthesis.

Design, Synthesis and Evaluation of a Series of 1,5‐Diaryl‐1,2,3‐triazole‐4‐carbohydrazones as Inhibitors of the YAP‐TAZ/TEAD Complex

B. Rubin, F. Bailly, A. Pobbati, 2021, ChemMedChem.

Monitoring of a three-step solid phase synthesis involving a Heck reaction using magic angle spinning NMR spectroscopy

G. Lippens, B. Déprez, P. Melnyk, 1996 .

High ligand efficiency quinazoline compounds as novel A2A adenosine receptor antagonists.

G. Han, V. Cherezov, S. Yous, 2022, European journal of medicinal chemistry.

A ß-Secretase Modulator Decreases Tau Pathology and Preserves Short-Term Memory in a Mouse Model of Neurofibrillary Degeneration

L. Buée, N. Sergeant, D. Blum, 2021, Frontiers in Pharmacology.

A β-secretase modulator decreases Tau pathology and preserves short-term memory in a mouse model of neurofibrillary degeneration

L. Buée, N. Sergeant, D. Blum, 2021, bioRxiv.

Recovery of brain biomarkers following peroxisome proliferator-activated receptor agonist neuroprotective treatment before ischemic stroke

L. Buée, R. Bordet, H. Drobecq, 2014, Proteome Science.

Synthesis and switching properties of new derivatives of azoresveratrol

B. Champagne, S. Delbaere, P. Melnyk, 2019 .

Buchwald reaction as the key step for the synthesis of metabolically more stable analogs of amodiaquine.

P. Melnyk, N. Le Fur, Paul-Emmanuel Larchanché, 2011, European journal of medicinal chemistry.

High‐affinity σ1 protein agonist reduces clinical and pathological signs of experimental autoimmune encephalomyelitis

P. Vermersch, A. Duhamel, P. Melnyk, 2015, British journal of pharmacology.

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.

L. Buée, N. Sergeant, V. Vingtdeux, 2018, European journal of medicinal chemistry.

Chloroquine and chloroquinoline derivatives as models for the design of modulators of amyloid Peptide precursor metabolism.

A. Delacourte, L. Buée, C. Sergheraert, 2015, ACS chemical neuroscience.

Quinazoline and phthalazine derivatives as novel melatonin receptor ligands analogues of agomelatine.

P. Delagrange, S. Yous, P. Melnyk, 2020, European journal of medicinal chemistry.

SK2 channels set a signalling hub bolstering CAF-triggered tumourigenic processes in pancreatic cancer

F. Bertucci, P. Finetti, R. Tomasini, 2022, Gut.

Safe and Efficient Sigma1 Ligand: A Potential Drug Candidate for Multiple Sclerosis

P. Vermersch, N. Duhal, P. Odou, 2022, International journal of molecular sciences.

Synthesis and pharmacological evaluation of dual ligands for melatonin (MT1/MT2) and serotonin 5-HT2C receptor subtypes (II).

J. Boutin, P. Delagrange, S. Yous, 2015, European journal of medicinal chemistry.

Synthesis and biological evaluation of new naphtho- and quinolinocyclopentane derivatives as potent melatoninergic (MT1/MT2) and serotoninergic (5-HT2C) dual ligands.

P. Delagrange, S. Yous, P. Melnyk, 2017, European journal of medicinal chemistry.

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

J. Boutin, P. Delagrange, S. Yous, 2017, European journal of medicinal chemistry.

Repositioning of FDA-Approved Antifungal Agents to Interrogate Acyl-CoA Synthetase Long Chain Family Member 4 (ACSL4) in Ferroptosis.

D. Devos, P. Melnyk, J. Devedjian, 2022, Biochemical pharmacology.

Tau pathology modulates Pin1 post-translational modifications and may be relevant as biomarker

L. Buée, I. Landrieu, G. Lippens, 2013, Neurobiology of Aging.

New phenylaniline derivatives as modulators of amyloid protein precursor metabolism.

L. Buée, N. Sergeant, S. Yous, 2018, Bioorganic & medicinal chemistry.

Probing the role of the covalent linkage of ferrocene into a chloroquine template.

C. Biot, D. Dive, B. Pradines, 2006, Journal of medicinal chemistry.

Synthesis and antimalarial evaluation of new N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.

C. Sergheraert, P. Melnyk, P. Grellier, 2005, Bioorganic & medicinal chemistry letters.

Crosstalk between the Hippo Pathway and the Wnt Pathway in Huntington’s Disease and Other Neurodegenerative Disorders

C. Simonin, P. Melnyk, M. Chartier-Harlin, 2022, Cells.

Heck reaction to a new heterocyclic system: pyrido[2′,3′-dt́]pyridazino[2,3-a]indole

P. Melnyk, J. Gasche, C. Thai, 1993 .

Improved synthesis of pyridazinediones under microwave irradiation

A. Tartar, P. Melnyk, L. Bourel, 1996 .

Exploring 6-(substituted sulfonyl)imidazopyridines as a potential scaffold for the design of 5-HT6 ligands

P. Melnyk, P. Carato, C. Furman, 2013, Monatshefte für Chemie - Chemical Monthly.

Methodology to Access Tetrahydrodipyridoimidazole Derivatives

P. Melnyk, P. Carato, M. Donnier-Maréchal, 2012 .

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.

X. Thuru, M. Lecoeur, P. Melnyk, 2016, Journal of medicinal chemistry.

Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.

P. Melnyk, P. Carato, M. Donnier-Maréchal, 2015, European journal of medicinal chemistry.

Design, synthesis and in vitro antimalarial activity of an acylhydrazone library.

C. Sergheraert, P. Melnyk, P. Grellier, 2006, Bioorganic & medicinal chemistry letters.

Optimized synthesis of tetrahydroisoquinoline-hydantoins

C. Sergheraert, P. Melnyk, Julie Charton, 2004 .

C. Korth, P. Melnyk, A. Ryckebusch, 2006, Journal of medicinal chemistry.

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

L. Buée, N. Sergeant, V. Vingtdeux, 2019, Neurobiology of Disease.

Pharmacomodulations around an anti-Alzheimer drug-candidate

P. Verwaerde, N. Sergeant, P. Melnyk, 2021, European Journal of Medicinal Chemistry Reports.

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.

J. Goossens, C. Danel, C. Vaccher, 2016, Journal of chromatography. A.

Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines.

L. Buée, P. Chavatte, D. Blum, 2015, European journal of medicinal chemistry.

Synthesis and antimalarial activity of new analogues of amodiaquine.

Philippe Grellier, C. Sergheraert, L. Maes, 2008, European journal of medicinal chemistry.

Design, synthesis and antimalarial activity of a glyoxylylhydrazone library.

C. Sergheraert, O. Melnyk, P. Melnyk, 2004, Bioorganic & medicinal chemistry letters.

Phenylthiocarbamate or N-Carbothiophenyl Group Chemistry in Peptide Synthesis and Bioconjugation

O. Melnyk, P. Melnyk, N. Ollivier, 2014, Bioconjugate chemistry.

Stereospecific pictet-spengler reaction: synthesis of cis (+)-(1S, 12bR)-1-aminoindoloquinolizidine from a pure α-(S)-aminoaldehyde derivative

P. Ducrot, P. Melnyk, C. Thal, 1993 .

Suzuki-miyaura cross-coupling reaction as the key step for the synthesis of some new 4'-aryl and alkyl substituted analogues of amodiaquine and amopyroquine

E. Pǎunescu, P. Melnyk, N. Matuszak, 2007 .

Effect of 6-Benzoyl-benzothiazol-2-one scaffold on the pharmacological profile of α-alkoxyphenylpropionic acid derived PPAR agonists

B. Staels, P. Melnyk, C. Dacquet, 2020, Journal of enzyme inhibition and medicinal chemistry.

Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 2.

C. Sergheraert, P. Melnyk, Julie Charton, 2005, Bioorganic & medicinal chemistry letters.

Replacement of the 4′‐Hydroxy Group of Amodiaquine and Amopyroquine by Aromatic and Aliphatic Substituents: Synthesis and Antimalarial Activity

E. Pǎunescu, P. Melnyk, P. Grellier, 2009, ChemMedChem.

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

J. Boutin, P. Delagrange, S. Yous, 2016, European journal of medicinal chemistry.

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

C. Supuran, J. Winum, S. Yous, 2019, Journal of enzyme inhibition and medicinal chemistry.

Design and synthesis of 2,6-disubstituted-8-amino imidazo[1,2a]pyridines, a promising privileged structure.

S. Yous, P. Melnyk, R. Boulahjar, 2018, Bioorganic & medicinal chemistry.

EGF-containing Membrane-bound Mucins: a hidden ErbB2 targeting pathway?

I. van Seuningen, P. Melnyk, Maxime Liberelle, 2020, Journal of medicinal chemistry.

Synthesis of new annelated indole systems: New entry in the E-azaeburnane series

P. Ducrot, B. Legrand, P. Melnyk, 1995 .

Heck Reaction to a New Heterocyclic System: Pyrido(2′,3′-d′)pyridazino( 2,3-a)indole.

P. Melnyk, C. Thal, J. Gasche, 1994 .

Non-Photoinduced Biological Properties of Verteporfin.

G. Huet, F. Bailly, P. Melnyk, 2016, Current medicinal chemistry.

Discovery of Compounds That Selectively Repress the Amyloidogenic Processing of the Amyloid Precursor Protein: Design, Synthesis and Pharmacological Evaluation of Diphenylpyrazoles

L. Buée, N. Sergeant, P. Melnyk, 2022, International journal of molecular sciences.

Thiocarbamate-Linked Polysulfonate–Peptide Conjugates As Selective Hepatocyte Growth Factor Receptor Binders

A. Romieu, O. Melnyk, H. Drobecq, 2014, Bioconjugate chemistry.

Recovery of brain biomarkers following peroxisome proliferator-activated receptor agonist neuroprotective treatment before ischemic stroke

L. Buée, R. Bordet, H. Drobecq, 2014, Proteome Science.

Progress with YAP/TAZ-TEAD inhibitors: a patent review (2018-present)

P. Melnyk, P. Cotelle, Benjamin Zagiel, 2022, Expert opinion on therapeutic patents.

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

P. Melnyk, R. Boulahjar, P. Carato, 2017, European journal of medicinal chemistry.

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

P. Melnyk, P. Carato, M. Donnier-Maréchal, 2015, European journal of medicinal chemistry.

Antagonists of the adenosine A2A receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity.

S. Yous, P. Melnyk, N. Renault, 2018, European journal of medicinal chemistry.

A Polyaminobiaryl-Based β-secretase Modulator Alleviates Cognitive Impairments, Amyloid Load, Astrogliosis, and Neuroinflammation in APPSwe/PSEN1ΔE9 Mice Model of Amyloid Pathology

N. Sergeant, P. Melnyk, Jamal El Bakali, 2023, International journal of molecular sciences.

6-Sulfonylbenzothiazolones as potential scaffolds for the design of 5-HT6 ligands.

P. Melnyk, P. Dallemagne, P. Carato, 2015, European journal of medicinal chemistry.

MUC4-ErbB2 Oncogenic Complex: Binding studies using Microscale Thermophoresis

X. Thuru, I. van Seuningen, C. Foulon, 2019, Scientific Reports.

Separation of Tic-hydantoin enantiomers, potent sigma-1 agonists, by high performance liquid chromatography and capillary electrophoresis.

C. Foulon, C. Vaccher, J. Bonte, 2010, Journal of chromatography. A.

Tic hydantoin sigma-1 agonist: Pharmacological characterization on cocaine-induced stimulant and appetitive effects

C. Foulon, C. Vaccher, P. Melnyk, 2009, European Neuropsychopharmacology.

Kinetics and mechanism of racemization of Tic-hydantoins, potent sigma-1 agonists

C. Foulon, C. Vaccher, J. Bonte, 2011 .

The EGF Domains of MUC4 Oncomucin Mediate HER2 Binding Affinity and Promote Pancreatic Cancer Cell Tumorigenesis

X. Thuru, I. van Seuningen, P. Melnyk, 2021, Cancers.

A new diastereoselective synthesis of (±) cis 1-aminoindoloquinolizidine

P. Ducrot, P. Melnyk, C. Thal, 1993 .

Targeting Transcriptional Enhanced Associate Domains (TEADs).

F. Bailly, P. Melnyk, P. Cotelle, 2017, Journal of medicinal chemistry.

Minimal chemical modification of reductive end of dextran to produce an amphiphilic polysaccharide able to incorporate onto lipid nanocapsules.

A. Barras, P. Melnyk, A. B. Younes, 2008, Bioconjugate chemistry.

Formulation and characterization of polyphenol-loaded lipid nanocapsules.

A. Barras, P. Melnyk, D. Betbeder, 2009, International journal of pharmaceutics.

A Phosphosite Mutant Approach on LRRK2 Links Phosphorylation and Dephosphorylation to Protective and Deleterious Markers, Respectively

X. Thuru, R. Nichols, T. Galli, 2022, Cells.

Combinatorial chemistry: A rational approach to chemical diversity

Dragos Horvath, Benoit Deprez, D. Horvath, 1996 .

1,4-bis(3-aminopropyl)piperazine libraries: from the discovery of classical chloroquine-like antimalarials to the identification of new targets.

P. Melnyk, R. Deprez-Poulain, 2005, Combinatorial chemistry & high throughput screening.

PM6280 and PM6577: ADME Study of Two Potent and Anti-malarial Amodiaquine Analogs with Improved Metabolic Stability

E. Pǎunescu, P. Melnyk, G. Hochart, 2015 .

Reviews : Journal of Medicinal & Organic Chemistry PM 6280 and PM 6577 : ADME Study of Two Potent and Anti-malarial Amodiaquine Analogs with Improved Metabolic Stability

E. Pǎunescu, P. Melnyk, G. Hochart, 2015 .

Optimized and convergent synthesis of potent anti-malarial aminoquinoline compounds: easy access to analogs

P. Melnyk, Paul-Emmanuel Larchanché, N. Fur, 2010 .

Synthesis and antimalarial activity of carbamate and amide derivatives of 4-anilinoquinoline.

C. Sergheraert, L. Maes, P. Melnyk, 2008, European journal of medicinal chemistry.

Synthesis and antimalarial activity of new amino analogues of amodiaquine.

E. Pǎunescu, P. Melnyk, P. Grellier, 2008, Medicinal chemistry (Shariqah (United Arab Emirates)).

Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.

C. Sergheraert, P. Melnyk, Julie Charton, 2005, Bioorganic & Medicinal Chemistry Letters.

Combinatorial chemistry: A rational approach to chemical diversity

Dragos Horvath, Benoit Deprez, D. Horvath, 1996 .

Tic hydantoin sigma-1 agonist: Pharmacological characterization on cocaine-induced stimulant and appetitive effects

C. Foulon, C. Vaccher, P. Melnyk, 2009, European Neuropsychopharmacology.