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Cyril PAPAMICAEL

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Straightforward Access to a New Class of Dual DYRK1A/CLK1 Inhibitors Possessing a Simple Dihydroquinoline Core

Mihaela-Liliana Ţînţaş , Ludovic Peauger , Florent Alix , Cyril Papamicaël , Thierry Besson
Molecules, 2023, 28 (1), pp.36. ⟨10.3390/molecules28010036⟩
Article dans une revue hal-03922046v1
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Design, Synthesis, and In Vitro Biological Activities of a Bio-Oxidizable Prodrug to Deliver Both ChEs and DYRK1A Inhibitors for AD Therapy

Anaïs Barré , Rabah Azzouz , Vincent Gembus , Cyril Papamicaël , Vincent Levacher
Molecules, 2019, 24 (7), pp.1264. ⟨10.3390/molecules24071264⟩
Article dans une revue hal-03134351v1
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Chemical Delivery System of MIBG to the Central Nervous System: Synthesis, 11 C-Radiosynthesis, and in Vivo Evaluation

Fabienne Gourand , Delphine Patin , Axelle Henry , Meźiane Ibazizeǹe , Martine Dhilly
ACS Medicinal Chemistry Letters, 2019, 10 (3), pp.352-357. ⟨10.1021/acsmedchemlett.8b00642⟩
Article dans une revue hal-03020265v1

Access to Highly Enantioenriched Donepezil-like 1,4-Dihydropyridines as Promising Anti-Alzheimer Prodrug Candidates via Enantioselective Tsuji Allylation and Organocatalytic Aza-Ene-Type Domino Reactions

Mihaela-Liliana Tîntas , R. Azzouz , L. Peauger , Vincent Gembus , Emilie Petit
Journal of Organic Chemistry, 2018, 83 (17), pp.10231-10240. ⟨10.1021/acs.joc.8b01442⟩
Article dans une revue hal-02024535v1

Dihydroquinoline Carbamate DQS1-02 as a Prodrug of a Potent Acetylcholinesterase Inhibitor for Alzheimer's Disease Therapy: Multigram-Scale Synthesis, Mechanism Investigations, in Vitro Safety Pharmacology, and Preliminary in Vivo Toxicology Profile

F. Alix , V. Gembus , L. Coquet , Marie Hubert-Roux , P. Chan
ACS Omega, 2018, 3 (12), pp.18387-18397. ⟨10.1021/acsomega.8b02121⟩
Article dans une revue hal-02024468v1
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Rational design of carbamate-based dual binding site and central AChE inhibitors by a “biooxidisable” prodrug approach: Synthesis, in vitro evaluation and docking studies

Mihaela-Liliana Ţînţaş , Vincent Gembus , Florent Alix , Anaïs Barré , Gaël Coadou
European Journal of Medicinal Chemistry, 2018, 155, pp.171-182. ⟨10.1016/j.ejmech.2018.05.057⟩
Article dans une revue hal-03134356v1

Rational design of carbamate-based dual binding site and central AChE inhibitors by a “biooxidisable” prodrug approach: Synthesis, in vitro evaluation and docking studies

Mihaela-Liliana Tîntas , Vincent Gembus , F. Alix , A. Barré , Gaël Coadou
European Journal of Medicinal Chemistry, 2018, 155, pp.171-182. ⟨10.1016/j.ejmech.2018.05.057⟩
Article dans une revue hal-02024536v1
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Dihydroquinoline Carbamate DQS1-02 as a Prodrug of a Potent Acetylcholinesterase Inhibitor for Alzheimer’s Disease Therapy: Multigram-Scale Synthesis, Mechanism Investigations, in Vitro Safety Pharmacology, and Preliminary in Vivo Toxicology Profile

Florent Alix , Vincent Gembus , Laurent Coquet , Marie Hubert-Roux , Philippe Chan
ACS Omega, 2018, 3 (12), pp.18387-18397. ⟨10.1021/acsomega.8b02121⟩
Article dans une revue hal-03134333v1

Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine “bio-oxidizable” prodrugs: Synthesis, biological evaluation and structure-activity relationship

Rabah Azzouz , Ludovic Peauger , Vincent Gembus , Mihaela-Liliana Tîntas , Jana Sopkova-de Oliveira Santos
European Journal of Medicinal Chemistry, 2018, 145, pp.165-190. ⟨10.1016/j.ejmech.2017.12.084⟩
Article dans une revue hal-02043695v1
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Access to Highly Enantioenriched Donepezil-like 1,4-Dihydropyridines as Promising Anti-Alzheimer Prodrug Candidates via Enantioselective Tsuji Allylation and Organocatalytic Aza-Ene-Type Domino Reactions

Mihaela-Liliana Ţînţaş , Rabah Azzouz , Ludovic Peauger , Vincent Gembus , Emilie Petit
Journal of Organic Chemistry, 2018, 83 (17), pp.10231-10240. ⟨10.1021/acs.joc.8b01442⟩
Article dans une revue hal-03134345v1

Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a “Bio-Oxidizable” Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation

Ludovic Peauger , Rabah Azzouz , Vincent Gembus , Mihaela-Liliana Ţînţaş , Jana Sopkova-de Oliveira Santos
Journal of Medicinal Chemistry, 2017, 60 (13), pp.5909-5926. ⟨10.1021/acs.jmedchem.7b00702⟩
Article dans une revue hal-02043729v1

Delivering FLT to the Central Nervous System by Means of a Promising Targeting System: Synthesis, [11C]Radiosynthesis, and in Vivo Evaluation

Fabienne Gourand , Mihaela-Liliana Tîntas , Axelle Henry , Méziane Ibazizène , Martine Dhilly
ACS Chemical Neuroscience, 2017, 8 (11), pp.2457-2467. ⟨10.1021/acschemneuro.7b00218⟩
Article dans une revue hal-02046279v1

An Overview of the Synthesis of Highly Versatile N-Hydroxysuccinimide Esters

Anaïs Barré , Mihaela-Liliana Tîntas , Vincent Levacher , Cyril Papamicaël , Vincent Gembus
Synthesis: Journal of Synthetic Organic Chemistry, 2017, 49 (3), pp.472-483. ⟨10.1055/s-0036-1588607⟩
Article dans une revue hal-02046258v1

The Influence of Amino Group Position on Aryl Moiety of SarAr on Metal Complexation and Protein Labelling

Vincent Jamier , Eskender Mume , Cyril Papamicaël , Suzanne V. Smith
Australian Journal of Chemistry, 2016, 69 (9), pp.1054-1061. ⟨10.1071/CH15794⟩
Article dans une revue hal-02046216v1

Dihydroquinoline Carbamate Derivatives as "Bio-oxidizable" Prodrugs for Brain Delivery of Acetylcholinesterase Inhibitors: [¹¹C] Radiosynthesis and Biological Evaluation

Pierre Bohn , F. Gourand , Cyril Papamicaël , M. Ibazizène , M Dhilly
ACS Chemical Neuroscience, 2015, 6 (5), pp.737-744. ⟨10.1021/cn5003539⟩
Article dans une revue hal-01578046v1

Palladium-Catalyzed Carbonylation of (Hetero)Aryl, Alkenyl and Allyl Halides by Means of N-Hydroxysuccinimidyl Formate as CO Surrogate

Anaïs Barré , Mihaela-Liliana Tîntas , Florent Alix , Vincent Gembus , Cyril Papamicaël
Journal of Organic Chemistry, 2015, 80 (13), pp.6537-6544. ⟨10.1021/acs.joc.5b01119⟩
Article dans une revue hal-02046139v1

Synthesis and Stability Evaluation of New HYNIC Derivatives as Ligands for Technetium-99m

Yoann Joyard , Laurent Bischoff , Vincent Levacher , Cyril Papamicaël , Pierre Vera
Letters in Organic Chemistry, 2014, 11 (3), pp.208-214. ⟨10.2174/15701786113106660087⟩
Article dans une revue hal-01141349v1

New developments in redox chemical delivery systems by means of 1,4-dihydroquinoline-based targetor: Application to galantamine delivery to the brain

Mihaela-Liliana Tîntas , Lénaïg Foucout , Sylvain Petit , Sylvain Oudeyer , Fabienne Gourand
European Journal of Medicinal Chemistry, 2014, 81, pp.218-226. ⟨10.1016/j.ejmech.2014.05.022⟩
Article dans une revue hal-01141464v1
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New developments in redox chemical delivery systems by means of 1,4-dihydroquinoline-based targetor: Application to galantamine delivery to the brain

Mihaela-Liliana Tîntas , Lénaïg Foucout , Sylvain Petit , Sylvain Oudeyer , Fabienne Gourand
European Journal of Medicinal Chemistry, 2014, 81, pp.218 - 226. ⟨10.1016/j.ejmech.2014.05.022⟩
Article dans une revue hal-03856118v1

Synthesis of sulfonic acid derivatives by oxidative deprotection of thiols using tert-butyl hypochlorite

Yoann Joyard , Cyril Papamicaël , Pierre Bohn , Laurent Bischoff
Organic Letters, 2013, 15 (9), pp.2294-2297. ⟨10.1021/ol400865b⟩
Article dans une revue hal-00997432v1

Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.

Yoann Joyard , Vadim Le Joncour , Hélène Castel , Chérif Bounana Diouf , Laurent Bischoff
Bioorganic and Medicinal Chemistry Letters, 2013, 23 (13), pp.3704-3708. ⟨10.1016/j.bmcl.2013.05.015⟩
Article dans une revue hal-00997430v1

Synthesis of new 18F-radiolabeled silicon-based nitroimidazole compounds.

Yoann Joyard , Rabah Azzouz , Laurent Bischoff , Cyril Papamicaël , Daniel Labar
Bioorganic and Medicinal Chemistry, 2013, 21 (13), pp.3680-3688. ⟨10.1016/j.bmc.2013.04.029⟩
Article dans une revue hal-00997431v1

Rational design of central selective acetylcholinesterase inhibitors by means of a "bio-oxidisable prodrug" strategy.

Pierre Bohn , Nicolas Le Fur , Guillaume Hagues , Jean Costentin , Nicolas Torquet
Organic & Biomolecular Chemistry, 2009, 7 (12), pp.2612-8. ⟨10.1039/b903041g⟩
Article dans une revue inserm-00467214v1

Synthesis of C1- and C3m-Symmetric Porphyrin Trimers Based on Triphenylmethane Cores

Cyril Papamicaël , Olivier Mongin , A. Gossauer
Chemical Monthly = Monatshefte für Chemie, 2007, 138 (8), pp.791-796. ⟨10.1007/s00706-007-0629-y⟩
Article dans une revue hal-00842774v1

Preparation of new axially chiral bridged 2,2′-bipyridines and pyridyl monooxazolines (pymox). Evaluation in copper( i )-catalyzed enantioselective cyclopropanation

Alexis Bouet , Barbara Heller , Cyril Papamicaël , Georges Dupas , Sylvain Oudeyer
Organic & Biomolecular Chemistry, 2007, 5 (9), pp.1397-1404. ⟨10.1039/b701549f⟩
Article dans une revue hal-02278796v1

A rapid synthesis of new benzene-centered porphyrin trimers.

C.A. Papamicaël , O. Mongin , A. Gossauer
J. Heterocyclic Chem., 2007, 44, pp.1071-1076
Article dans une revue hal-00323063v1

Synthesis of C1- and C3v-Symmetric Porphyrin Trimers Based on Triphenylmethane Cores

C.A. Papamicaël , O. Mongin , A. Gossauer
Chemical Monthly = Monatshefte für Chemie, 2007, 138, pp.791-796
Article dans une revue hal-00323182v1

New development of meyers' methodology : stereoselective preparation of an axially chiral 5,7-fused bicyclic lactam related to circumdatins/benzomalvins and asperlicins.

M. Penhoat , Pierre Bohn , G. Dupas , C. Papamicaël , Francis Marsais
Tetrahedron: Asymmetry, 2006, pp.281-6
Article dans une revue hal-00475867v1
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Solid phase synthesis of a redox delivery system with the aim of targeting peptides into the brain.

Claudine Patteux , Lénaïg Foucout , Pierre Bohn , Georges Dupas , Jérôme Leprince
Organic & Biomolecular Chemistry, 2006, 4 (5), pp.817-25. ⟨10.1039/b516737j⟩
Article dans une revue inserm-00475858v1

Synthesis of Various Terphenyl Derivatives; Study of a New Amine Receptor with a Terphenyl Structure

Patricia Le Nahenec-Martel , Stéphane Leleu , Francis Marsais , Cyril Papamicaël , Vincent Levacher
Letters in Organic Chemistry, 2005, 2 (2), pp.172-175. ⟨10.2174/1570178053202955⟩
Article dans une revue hal-02547629v1

Chemoselective, accelerated and stereoselective aza-Michael addition of amines to N-phenylmaleimide by using TMEDA based receptors

Yuefeng Bi , Laëtitia Bailly , Francis Marsais , Vincent Levacher , Cyril Papamicaël
Tetrahedron: Asymmetry, 2004, 15 (23), pp.3703-3706. ⟨10.1016/j.tetasy.2004.10.006⟩
Article dans une revue hal-02378309v1
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The Inhibitor Thiomandelic Acid Binds to Both Metal Ions in Metallo-β-lactamase and Induces Positive Cooperativity in Metal Binding

Christian Damblon , Mikael Jensen , Abdessamad Ababou , Igor Barsukov , Cyril Papamicaël
Journal of Biological Chemistry, 2003, 278 (31), pp.29240-29251. ⟨10.1074/jbc.M301562200⟩
Article dans une revue hal-03856336v1
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Three-dimensional Structure of FEZ-1, a Monomeric Subclass B3 Metallo-β-lactamase from Fluoribacter gormanii, in Native Form and in Complex with d-Captopril

I Garcı́a-Sáez , P S Mercuri , Cyril Papamicaël , R Kahn , J M Frère
Journal of Molecular Biology, 2003, 325, pp.651 - 660. ⟨10.1016/s0022-2836(02)01271-8⟩
Article dans une revue hal-03856347v1
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The 1.5-Å structure of $Chryseobacterium\ meningosepticum$ zinc β-lactamase in complex with the inhibitor, D-Captopril

Isabel García-Sáez , Julie Hopkins , Cyril Papamicaël , Nicola Franceschini , Gianfranco Amicosante
Journal of Biological Chemistry, 2003, 278, pp.23868 - 23873. ⟨10.1074/jbc.m301062200⟩
Article dans une revue hal-03856326v1
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Thiomandelic Acid, a Broad Spectrum Inhibitor of Zinc β-Lactamases

Claire Mollard , Catherine Moali , Cyril Papamicaël , Christian Damblon , Sandrine Vessilier
Journal of Biological Chemistry, 2001, 276 (48), pp.45015 - 45023. ⟨10.1074/jbc.m107054200⟩
Article dans une revue hal-03856340v1

Thiomandelic acid, a broad spectrum inhibitor of zinc beta-lactamases: kinetic and spectroscopic studies.

C. Mollard , C. Moali , C. Papamicael , C. Damblon , S. Vessilier
Journal of Biological Chemistry, 2001, 276, pp.45015-45023
Article dans une revue hal-00314477v1

Vectorisation of [18F] radiotracers for brain tumors imaging

M-L Tintas , A Henry , S Guillouet , M Ibazizène , M Dhilly
5th World Congress & Expo on Pharmaceutics & Drug Delivery Systems, Feb 2020, Lisbonne, Portugal
Communication dans un congrès hal-02489363v1

Vectorisation cérébrale de la [18F]FLT pour l’imagerie de gliomes de bas grade.

Ml. Tintas , S. Guillouet , M. Ibazizène , M. Dhilly , F. . Fillesoye
24th Young Research Fellow Meeting in Medicinal Chemistry, Feb 2017, Châtenay-Malabry, France
Communication dans un congrès hal-02320458v1

Promising chemical delivery system into the central nervous system of [18F]FLT for PET imaging studies of low-grade brain tumours.

F. Gourand , A. Henry , M. Ibazizene , M. Dhilly , Cyril Papamicaël
Annual Congress of the European-Association-of-Nuclear-Medicine (EANM, 28, 2015), Oct 2015, Hambourg, Germany. pp.476-477
Communication dans un congrès hal-02024980v1

New developments for targeting drugs into central nervous system by means of a redox chemical delivery system

Cyril Papamicaël
Conference on organic chemistry (COC), Jun 2015, Suzhou, China
Communication dans un congrès hal-02384624v1

New Developments for Targeting Drugs into Central Nervous System by Means of a Redox Chemical Delivery System

C Papamicaël , V Levacher , F Gourand , L Barré
International Conference on Organic Chemistry, Jun 2015, ShanghaÏ, China
Communication dans un congrès hal-02488939v1

Synthesis of Technidazole: a potential new 99mTc ligand for imaging tumor hypoxia

Yoann Joyard , Pierre Bohn , Cyril Papamicaël , Vincent Levacher , Pierre Vera
Annual Congress of the European Association of Nuclear Medicine, 2012, Milan, Italy
Communication dans un congrès hal-01154357v1

Synthèse de radiomarqueurs technétiés et fluorés pour la détection de cellules hypoxiques tumorales

Y. Joyard , R. Azzouz , C. Fruit , L. Bischoff , C. Papamicael
4èmes journées scientifiques du cancéropôle nord-ouest, May 2011, Deauville, France
Communication dans un congrès hal-00673945v1

Transport into the central nervous system of [18F]FLT and [18F]Fludarabine for brain tumors

M-L Tintas , S Guillouet , M Ibazizène , F Fillesoye , C Papamicaël
4th Nuclear Technologies for Health Symposium, NTHS2020, Feb 2020, Nantes, France
Poster de conférence hal-02487617v1

Transport into the central nervous system of [18F]FLT and [18F]Fludarabine for brain tumors

Mihaela-Liliana Tîntas , S Guillouet , Méziane Ibazizène , Fabien Fillesoye , C. Papamicaël
23rd International Symposium on Radiopharmaceutical Sciences, May 2019, Beijing, China
Poster de conférence hal-02374599v1

Development of new redox chemical delivery systems for targeting radiotracers into the brain

A Henry , C Papamicaël , D Patin , F Gourand , L Barré
Journée de l’Ecole Doctorale Normande de Chimie (JEDNC), Jun 2016, Caen, France
Poster de conférence hal-02386584v1

New redox chemical delivery systems to target radiotracers into the brain

A Henry , P Papamicaël , D Patin , F Gourand , L Barré
52èmes Rencontres Internationales de Chimie Thérapeutique, Jul 2016, Caen, France
Poster de conférence hal-02386568v1

Dihydroquinoline derivatives as redox chemical delivery systems (CDS) or “bio-oxidisable” prodrugs for brain delivery of acetylcholinesterase inhibitors : design, synthesis, [11C] radiosynthesis and biological evaluation

P Bohn , F Gourand , C Papamicaël , M Ibazizène , M Dhilly
XVI International Conference on Heterocycles in Bioorganic Chemistry, Jun 2015, Metz, France
Poster de conférence hal-02386824v1

Dihydroquinoline derivatives as redox chemical delivery systems (CDS) or “bio-oxidisable” prodrugs for brain delivery of acetylcholinesterase inhibitors: design, synthesis, [11C]radiosynthesis and biological evaluation

P Bohn , F Gourand , C Papamicaël , M Ibazizène , M Dhilly
Journées Neurosciences, Workshop FLI, Nov 2015, Orsay, France
Poster de conférence hal-02386737v1

Development of redox chemical delivery systems for targeting radiotracers in central nervous system

A Henry , C Papamicaël , V Levacher , D Patin , F Gourand
Journées Nord-Ouest Européennes des Jeunes Chercheurs (JNOEJC), May 2015, Rouen, France
Poster de conférence hal-02386797v1

Promising chemical delivery system into the central nervous system of [18F]FLT for PET imaging studies  of low-grade brain tumours

F Gourand , A Henry , M Ibazizène , M Dhilly , C Papamicaël
Congrès EANM15, Oct 2015, Hambourg, Germany
Poster de conférence hal-02386810v1