essai

Anaïs Barré, Rabah Azzouz, Vincent Gembus, Cyril Papamicaël, Vincent Levacher. Design, Synthesis, and In Vitro Biological Activities of a Bio-Oxidizable Prodrug to Deliver Both ChEs and DYRK1A Inhibitors for AD Therapy. Molecules, MDPI, 2019, 24 (7), pp.1264. ⟨10.3390/molecules24071264⟩. ⟨hal-03134351⟩

Fabienne Gourand, Delphine Patin, Axelle Henry, Meźiane Ibazizeǹe, Martine Dhilly, et al.. Chemical Delivery System of MIBG to the Central Nervous System: Synthesis, 11 C-Radiosynthesis, and in Vivo Evaluation. ACS Medicinal Chemistry Letters, American Chemical Society, 2019, 10 (3), pp.352-357. ⟨10.1021/acsmedchemlett.8b00642⟩. ⟨hal-03020265⟩

Anaïs Barré, Rabah Azzouz, Vincent Gembus, Cyril Papamicaël, Vincent Levacher. Design, Synthesis, and In Vitro Biological Activities of a Bio-Oxidizable Prodrug to Deliver Both ChEs and DYRK1A Inhibitors for AD Therapy. Molecules, MDPI, 2019, 24 (7), pp.1264. ⟨10.3390/molecules24071264⟩. ⟨hal-03020280⟩

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

Mihaela-Liliana Tîntas, Vincent Gembus, F. Alix, A. Barré, Gaël Coadou, et al.. Rational design of carbamate-based dual binding site and central AChE inhibitors by a “biooxidisable” prodrug approach: Synthesis, in vitro evaluation and docking studies. European Journal of Medicinal Chemistry, Elsevier, 2018, 155, pp.171-182. ⟨10.1016/j.ejmech.2018.05.057⟩. ⟨hal-02024536⟩

Mihaela-Liliana Tîntas, R. Azzouz, L. Peauger, Vincent Gembus, Emilie Petit, et al.. 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. Journal of Organic Chemistry, American Chemical Society, 2018, 83 (17), pp.10231-10240. ⟨10.1021/acs.joc.8b01442⟩. ⟨hal-02024535⟩

Mihaela-Liliana Ţînţaş, Rabah Azzouz, Ludovic Peauger, Vincent Gembus, Emilie Petit, et al.. 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. Journal of Organic Chemistry, American Chemical Society, 2018, 83 (17), pp.10231-10240. ⟨10.1021/acs.joc.8b01442⟩. ⟨hal-03134345⟩

Rabah Azzouz, Ludovic Peauger, Vincent Gembus, Mihaela-Liliana Tîntas, Jana Sopkova-de Oliveira Santos, et al.. Novel donepezil-like N-benzylpyridinium salt derivatives as AChE inhibitors and their corresponding dihydropyridine “bio-oxidizable” prodrugs: Synthesis, biological evaluation and structure-activity relationship. European Journal of Medicinal Chemistry, Elsevier, 2018, 145, pp.165-190. ⟨10.1016/j.ejmech.2017.12.084⟩. ⟨hal-02043695⟩

F. Alix, V. Gembus, L. Coquet, Marie Hubert-Roux, P. Chan, et al.. 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. ACS Omega, ACS Publications, 2018, 3 (12), pp.18387-18397. ⟨10.1021/acsomega.8b02121⟩. ⟨hal-02024468⟩

Mihaela-Liliana Ţînţaş, Vincent Gembus, Florent Alix, Anaïs Barré, Gaël Coadou, et al.. Rational design of carbamate-based dual binding site and central AChE inhibitors by a “biooxidisable” prodrug approach: Synthesis, in vitro evaluation and docking studies. European Journal of Medicinal Chemistry, Elsevier, 2018, 155, pp.171-182. ⟨10.1016/j.ejmech.2018.05.057⟩. ⟨hal-03134356⟩

Ludovic Peauger, Rabah Azzouz, Vincent Gembus, Mihaela-Liliana Ţînţaş, Jana Sopkova-de Oliveira Santos, et al.. Donepezil-Based Central Acetylcholinesterase Inhibitors by Means of a “Bio-Oxidizable” Prodrug Strategy: Design, Synthesis, and in Vitro Biological Evaluation. Journal of Medicinal Chemistry, American Chemical Society, 2017, 60 (13), pp.5909-5926. ⟨10.1021/acs.jmedchem.7b00702⟩. ⟨hal-02043729⟩

Anaïs Barré, Mihaela-Liliana Tîntas, Vincent Levacher, Cyril Papamicaël, Vincent Gembus. An Overview of the Synthesis of Highly Versatile N-Hydroxysuccinimide Esters. Synthesis: Journal of Synthetic Organic Chemistry, Georg Thieme Verlag, 2017, 49 (3), pp.472-483. ⟨10.1055/s-0036-1588607⟩. ⟨hal-02046258⟩

Fabienne Gourand, Mihaela-Liliana Tîntas, Axelle Henry, Méziane Ibazizène, Martine Dhilly, et al.. Delivering FLT to the Central Nervous System by Means of a Promising Targeting System: Synthesis, [11C]Radiosynthesis, and in Vivo Evaluation. ACS Chemical Neuroscience, American Chemical Society (ACS), 2017, 8 (11), pp.2457-2467. ⟨10.1021/acschemneuro.7b00218⟩. ⟨hal-02046279⟩

Vincent Jamier, Eskender Mume, Cyril Papamicaël, Suzanne V. Smith. The Influence of Amino Group Position on Aryl Moiety of SarAr on Metal Complexation and Protein Labelling. Australian Journal of Chemistry, CSIRO Publishing, 2016, 69 (9), pp.1054-1061. ⟨10.1071/CH15794⟩. ⟨hal-02046216⟩

Pierre Bohn, F. Gourand, Cyril Papamicaël, M. Ibazizène, M Dhilly, et al.. Dihydroquinoline Carbamate Derivatives as "Bio-oxidizable" Prodrugs for Brain Delivery of Acetylcholinesterase Inhibitors: [¹¹C] Radiosynthesis and Biological Evaluation. ACS Chemical Neuroscience, American Chemical Society (ACS), 2015, 6 (5), pp.737-744. ⟨10.1021/cn5003539⟩. ⟨hal-01578046⟩

Anaïs Barré, Mihaela-Liliana Tîntas, Florent Alix, Vincent Gembus, Cyril Papamicaël, et al.. Palladium-Catalyzed Carbonylation of (Hetero)Aryl, Alkenyl and Allyl Halides by Means of N-Hydroxysuccinimidyl Formate as CO Surrogate. Journal of Organic Chemistry, American Chemical Society, 2015, 80 (13), pp.6537-6544. ⟨10.1021/acs.joc.5b01119⟩. ⟨hal-02046139⟩

Yoann Joyard, Laurent Bischoff, Vincent Levacher, Cyril Papamicaël, Pierre Vera, et al.. Synthesis and Stability Evaluation of New HYNIC Derivatives as Ligands for Technetium-99m. Letters in Organic Chemistry, Bentham Science Publishers, 2014, 11 (3), pp.208-214. ⟨10.2174/15701786113106660087⟩. ⟨hal-01141349⟩

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

Yoann Joyard, Vadim Le Joncour, Hélène Castel, Chérif Bounana Diouf, Laurent Bischoff, et al.. Synthesis and biological evaluation of a novel (99m)Tc labeled 2-nitroimidazole derivative as a potential agent for imaging tumor hypoxia.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2013, 23 (13), pp.3704-3708. ⟨10.1016/j.bmcl.2013.05.015⟩. ⟨hal-00997430⟩

Yoann Joyard, Cyril Papamicaël, Pierre Bohn, Laurent Bischoff. Synthesis of sulfonic acid derivatives by oxidative deprotection of thiols using tert-butyl hypochlorite. Organic Letters, American Chemical Society, 2013, 15 (9), pp.2294-2297. ⟨10.1021/ol400865b⟩. ⟨hal-00997432⟩

Yoann Joyard, Rabah Azzouz, Laurent Bischoff, Cyril Papamicaël, Daniel Labar, et al.. Synthesis of new 18F-radiolabeled silicon-based nitroimidazole compounds.. Bioorganic and Medicinal Chemistry, Elsevier, 2013, 21 (13), pp.3680-3688. ⟨10.1016/j.bmc.2013.04.029⟩. ⟨hal-00997431⟩

Pierre Bohn, Nicolas Le Fur, Guillaume Hagues, Jean Costentin, Nicolas Torquet, et al.. Rational design of central selective acetylcholinesterase inhibitors by means of a "bio-oxidisable prodrug" strategy.. Organic & Biomolecular Chemistry, Royal Society of Chemistry, 2009, 7 (12), pp.2612-8. ⟨10.1039/b903041g⟩. ⟨inserm-00467214⟩

Cyril Papamicaël, Olivier Mongin, A. Gossauer. Synthesis of C1- and C3m-Symmetric Porphyrin Trimers Based on Triphenylmethane Cores. Chemical Monthly = Monatshefte für Chemie, Springer Verlag, 2007, 138 (8), pp.791-796. ⟨10.1007/s00706-007-0629-y⟩. ⟨hal-00842774⟩

Alexis Bouet, Barbara Heller, Cyril Papamicaël, Georges Dupas, Sylvain Oudeyer, et al.. Preparation of new axially chiral bridged 2,2′-bipyridines and pyridyl monooxazolines (pymox). Evaluation in copper( i )-catalyzed enantioselective cyclopropanation. Organic & Biomolecular Chemistry, Royal Society of Chemistry, 2007, 5 (9), pp.1397-1404. ⟨10.1039/b701549f⟩. ⟨hal-02278796⟩

C.A. Papamicaël, O. Mongin, A. Gossauer. Synthesis of C1- and C3v-Symmetric Porphyrin Trimers Based on Triphenylmethane Cores. Chemical Monthly = Monatshefte für Chemie, Springer Verlag, 2007, 138, pp.791-796. ⟨hal-00323182⟩

C.A. Papamicaël, O. Mongin, A. Gossauer. A rapid synthesis of new benzene-centered porphyrin trimers.. J. Heterocyclic Chem., 2007, 44, pp.1071-1076. ⟨hal-00323063⟩

Claudine Patteux, Lénaïg Foucout, Pierre Bohn, Georges Dupas, Jérôme Leprince, et al.. Solid phase synthesis of a redox delivery system with the aim of targeting peptides into the brain.. Organic & Biomolecular Chemistry, Royal Society of Chemistry, 2006, 4 (5), pp.817-25. ⟨10.1039/b516737j⟩. ⟨inserm-00475858⟩

M. Penhoat, Pierre Bohn, G. Dupas, C. Papamicaël, Francis Marsais, et al.. New development of meyers' methodology : stereoselective preparation of an axially chiral 5,7-fused bicyclic lactam related to circumdatins/benzomalvins and asperlicins.. Tetrahedron: Asymmetry, Elsevier, 2006, pp.281-6. ⟨hal-00475867⟩

Patricia Le Nahenec-Martel, Stéphane Leleu, Francis Marsais, Cyril Papamicaël, Vincent Levacher, et al.. Synthesis of Various Terphenyl Derivatives; Study of a New Amine Receptor with a Terphenyl Structure. Letters in Organic Chemistry, Bentham Science Publishers, 2005, 2 (2), pp.172-175. ⟨10.2174/1570178053202955⟩. ⟨hal-02547629⟩

Yuefeng Bi, Laëtitia Bailly, Francis Marsais, Vincent Levacher, Cyril Papamicaël, et al.. Chemoselective, accelerated and stereoselective aza-Michael addition of amines to N-phenylmaleimide by using TMEDA based receptors. Tetrahedron: Asymmetry, Elsevier, 2004, 15 (23), pp.3703-3706. ⟨10.1016/j.tetasy.2004.10.006⟩. ⟨hal-02378309⟩

C. Mollard, C. Moali, C. Papamicael, C. Damblon, S. Vessilier, et al.. Thiomandelic acid, a broad spectrum inhibitor of zinc beta-lactamases: kinetic and spectroscopic studies.. Journal of Biological Chemistry, American Society for Biochemistry and Molecular Biology, 2001, 276, pp.45015-45023. ⟨hal-00314477⟩

M-L Tintas, A Henry, S Guillouet, M Ibazizène, M Dhilly, et al.. Vectorisation of [18F] radiotracers for brain tumors imaging. 5th World Congress & Expo on Pharmaceutics & Drug Delivery Systems, Feb 2020, Lisbonne, Portugal. ⟨hal-02489363⟩

Ml. Tintas, S. Guillouet, M. Ibazizène, M. Dhilly, F. . Fillesoye, et al.. Vectorisation cérébrale de la [18F]FLT pour l’imagerie de gliomes de bas grade.. 24th Young Research Fellow Meeting in Medicinal Chemistry, Feb 2017, Châtenay-Malabry, France. ⟨hal-02320458⟩

C Papamicaël, V Levacher, F Gourand, L Barré. New Developments for Targeting Drugs into Central Nervous System by Means of a Redox Chemical Delivery System. International Conference on Organic Chemistry, Jun 2015, ShanghaÏ, China. ⟨hal-02488939⟩

F. Gourand, A. Henry, M. Ibazizene, M. Dhilly, Cyril Papamicaël, et al.. Promising chemical delivery system into the central nervous system of [18F]FLT for PET imaging studies of low-grade brain tumours.. Annual Congress of the European-Association-of-Nuclear-Medicine (EANM, 28, 2015), Oct 2015, Hambourg, Germany. pp.476-477. ⟨hal-02024980⟩

Cyril Papamicaël. New developments for targeting drugs into central nervous system by means of a redox chemical delivery system. Conference on organic chemistry (COC), Jun 2015, Suzhou, China. ⟨hal-02384624⟩

Yoann Joyard, Pierre Bohn, Cyril Papamicaël, Vincent Levacher, Pierre Vera. Synthesis of Technidazole: a potential new 99mTc ligand for imaging tumor hypoxia. Annual Congress of the European Association of Nuclear Medicine, 2012, Milan, Italy. ⟨hal-01154357⟩

Y. Joyard, R. Azzouz, C. Fruit, L. Bischoff, C. Papamicael, et al.. Synthèse de radiomarqueurs technétiés et fluorés pour la détection de cellules hypoxiques tumorales. 4èmes journées scientifiques du cancéropôle nord-ouest, May 2011, Deauville, France. ⟨hal-00673945⟩

M-L Tintas, S Guillouet, M Ibazizène, F Fillesoye, C Papamicaël, et al.. Transport into the central nervous system of [18F]FLT and [18F]Fludarabine for brain tumors. 4th Nuclear Technologies for Health Symposium, NTHS2020, Feb 2020, Nantes, France. ⟨hal-02487617⟩

Mihaela-Liliana Tîntas, S Guillouet, Méziane Ibazizène, Fabien Fillesoye, C. Papamicaël, et al.. Transport into the central nervous system of [18F]FLT and [18F]Fludarabine for brain tumors. 23rd International Symposium on Radiopharmaceutical Sciences, May 2019, Beijing, China. ⟨hal-02374599⟩

A Henry, C Papamicaël, D Patin, F Gourand, L Barré, et al.. Development of new redox chemical delivery systems for targeting radiotracers into the brain. Journée de l’Ecole Doctorale Normande de Chimie (JEDNC), Jun 2016, Caen, France. ⟨hal-02386584⟩

A Henry, P Papamicaël, D Patin, F Gourand, L Barré, et al.. New redox chemical delivery systems to target radiotracers into the brain. 52èmes Rencontres Internationales de Chimie Thérapeutique, Jul 2016, Caen, France. ⟨hal-02386568⟩

A Henry, C Papamicaël, V Levacher, D Patin, F Gourand, et al.. Development of redox chemical delivery systems for targeting radiotracers in central nervous system. Journées Nord-Ouest Européennes des Jeunes Chercheurs (JNOEJC), May 2015, Rouen, France. ⟨hal-02386797⟩

P Bohn, F Gourand, C Papamicaël, M Ibazizène, M Dhilly, et al.. 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. Journées Neurosciences, Workshop FLI, Nov 2015, Orsay, France. ⟨hal-02386737⟩

P Bohn, F Gourand, C Papamicaël, M Ibazizène, M Dhilly, et al.. 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. XVI International Conference on Heterocycles in Bioorganic Chemistry, Jun 2015, Metz, France. ⟨hal-02386824⟩

F Gourand, A Henry, M Ibazizène, M Dhilly, C Papamicaël, et al.. Promising chemical delivery system into the central nervous system of [18F]FLT for PET imaging studies  of low-grade brain tumours. Congrès EANM15, Oct 2015, Hambourg, Germany. ⟨hal-02386810⟩