DUBOST Emmanuelle [email protected] Nationality
Transcription
DUBOST Emmanuelle [email protected] Nationality
DUBOST Emmanuelle [email protected] Nationality: French Date and place of birth: August 22nd, 1984 (Bayeux) Experiences 2016-today Post-doctoral position: Centre d’Etudes et de Recherche sur le Médicament de Normandie (CERMN)- Caen C-H radio-iodination of (bio)molecules Supervisor: Dr. Thomas Cailly ([email protected]) 2014-2015 Post-doctoral position: Chemistry Research Laboratory (CRL) – University of Oxford – United Kingdom Towards access to trifluorinated and perfluorinated alkyl compounds - Radiosynthesis of PET biomarker [18F]EF5 from fluoride ARC grant and Marie-Curie fellowship Supervisor: Pr. Véronique Gouverneur ([email protected]) 2012-2014 Post-doctoral position - Comissariat à l’Energie Atomique (CEA)-Saclay-France Synthesis of new cryptophanes as biosensors for 129Xe MRI of oxidative stress Supervisor: Dr. B. Rousseau (01.69.08.25.70 - [email protected]) 2011 (4 months) Post-doctoral position – CERMN- Caen Development of new Multi Target Directed Ligands (MTDLs) with both anti-acetylcholinesterase and serotoninergic 5-HT4 receptor agonist activities for the treatment of Alzheimer’s disease Supervisor: Pr. P. Dallemagne (02.31.56.68.13 - [email protected]) (8 months) Research assistant in analytical and medicinal chemistry - Caen Development of a new and direct synthesis of substituted indazoles Supervisor: Pr. V. Collot (02.31.56.68.15 – [email protected]) 2007-2010 Ph. D. in Organic and medicinal chemistry - CERMN- University of Caen Developement of an efficient access to substituted phenanthridin-6(5H)-ones using Suzuki-Miyaura crosscoupling and anionic ring closure Development of a regioselective ortho-monobromination of benzaldoximes through palladium catalyzed C-H activation Application of these methodologies on the synthesis of 5-HT4 receptors ligands. Ph. D. Supervisor: Pr. F. Fabis (02.31.56.68.08 – [email protected]) 2007 (6 months) Training course - Laboratoire de Chimie Moléculaire et Thio-organique (LCMT) -Caen Organocatalysed synthesis of Imperanene- Application of asymetric decarboxylation Supervisor: Pr. J. Rouden (02 31 45 28 93 – [email protected]) 2006 (10 weeks) Training course – CERMN – Caen Synthesis of 7-piperazinylsteroids as anticancer agent Supervisor: Pr. L. El Kihel (02.31.56.68.12 - [email protected]) Academic achievements and others informations 2015 2011 (8 months) Tutorials in organic chemistry – Merton College – University of Oxford Teaching and research assistant in analytical and medicinal chemistry – Caen Practical works of analytical and medicinal chemistry for students in Pharmacy, 2009 (6 months) Teaching and research assistant in medicinal chemistry – Caen Practical works of organic and medicinal chemistry for students in Pharmacy Supervision of 8 students: 2A pharmacy, L2 DUT chemistry, 2* M1 chemistry, 3*M2 chemistry or equivalent, D3 Funding: Writing of French (ARC, FRM) and European (Marie Curie fellowship) funding proposals - 2 successful. Education 2007-2010 Ph. D. in Organic and medicinal chemistry - CERMN- University of Caen Conception, synthesis and biological study of new phenanthridines as serotoninergic receptor 5-HT4 ligands 2002-2007 2002 Master Research Diploma in Organic Chemistry - University of Caen Baccalauréat in Science, option Physique-Chimie - Lycée Jean-François Millet - Cherbourg Publications 10. O’Duill, M.; Dubost, E.; Pfeifer, L. ; Gouverneur, V. Cross-Coupling of [2-Aryl-1,1,2,2tetrafluoroethyl]trimethylsilanes with Aryl Halides. Org. Lett. 2015, 17(14), 3466-3469. 9. Kotera, N.; Dubost, E.; Milanole, G.; Doris, E.; Gravel, E.; Arhel, N.; Brotin, T.; Dutasta, J.-P.; Cochrane, J.; Mari, E.; Boutin, C.; Leonce, E.; Berthault, P .; Rousseau, B. A doubly smart probe for the detection of Cys4-tagged proteins. Chem. Commun. 2015, 51, 11482-11484.. 8. Rochais, C. ;Lecoutey, C. ; Gaven, F. ;Giannoni, P. ; Hamidouche, K. ; Hedou, D. ; Dubost, E.; Genest, D.; Yahiaoui, S.; Freret, T.; Bouet, V.; Dauphin, F. ; Sopkova-de Oliveira Santos, J. ; Ballandonne, C. ; Corvaisier, S. ; MalzertFréon, A. ; Legay, R. ; Boulouard, M. ; Claeysen, S. ; Dallemagne, P. Novel MTDLs with AChE inhibitory and 5-HT4R agonist activities as potential agents against Alzheimer’s disease: the design of donecopride. J. Med. Chem. 2015, 58, 3172−3187. 7. Dubost, E.; Stiebing, S.; Ferrary, T.; Cailly, T.; Fabis, F.; Collot, V. A general synthesis of diversely substituted indazoles and heteroaromatic derivatives from o-halo-(het)arylaldehydes or –phenones. Tetrahedron 2014, 70, 8413-8418. 6. Dubost, E.; Dognon, J.-P.; Rousseau, B.; Milanole, G.; Dugave, C.; Boulard, Y.; Léonce, E.; Boutin, C.; Berthault, P. Understanding a Host–Guest Model System through 129Xe NMR Spectroscopic Experiments and Theoretical Studies. Angew. Chem. Int. Ed. 2014, 53, 9837–9840. 5. Tassali, N.; Kotera, N.; Boutin, C.; Léonce, E.; Boulard, Y.; Rousseau, B.; Dubost, E.; Taran, F.; Brotin, B.; Dutasta, J.-P.; Berthault, P. Smart Detection of Toxic Metal Ions, Pb2+ and Cd2+, using a 129Xe NMR-based Sensor. Anal. Chem. 2014, 86, 1783-1788. 4. Dubost, E.; Kotera, N. ; Garcia-Argote, S. ; Boulard, Y. ; Léonce, E.; Boutin, C.; Berthault, P.; Dugave, C.; Rousseau, B. Synthesis of a functionalizable water-soluble cryptophane-111. Org. Lett. 2013, 15, 2866–2868. 3. Dubost, E. ; Dumas, N.; Fossey, C.; Magnelli, R.; Butt, S.; Ballandonne, C.; Caignard, D.H.; Dulin, F. ; Sopkovade Oliveira Santos, J. ; Millet, P. ; Charnay, Y. ; Rault, S. ; Cailly, T.; Fabis, F. Synthesis and Structure-Affinity Relationships of Selective High-Affinity 5-HT4 Receptor Antagonists: Application to the Design of New Potential Single Photon Emission Computed Tomography (SPECT) Tracers. J. Med. Chem. 2012, 55, 9693-9707. 2. Dubost, E.; Fossey, C.; Cailly, T.; Rault, S.; Fabis, F. Selective ortho-bromination of substituted benzaldoximes using Pd-catalyzed C-H activation: application to the synthesis of substituted 2-bromobenzaldehydes. J. Org. Chem. 2011, 76, 6414-6420. 1. Dubost, E.; Magnelli, R.; Cailly, T.; Legay, R.; Fabis, F.; Rault, S. General method for the synthesis of substituted phenanthridin-6(5H)-ones using a KOH-mediated anionic ring closure as the key step. Tetrahedron 2010, 66, 5008-5016. Oral communications 6. Conception and synthesis of cryptophanes for hyperpolarized 129Xe MRI. Oxford Cancer Imaging Center seminar, 2015, Oxford, United Kingdom. 5. Selective ortho-bromination of substituted benzaldoximes. Application to the synthesis of substituted 2bromobenzaldehydes. Groupement des Pharmacochimistes de l’Arc Atlantique (GP2A), 2011, Cork, Ireland. 4. Synthesis of new 5-HT4 receptors ligands through palladium catalyzed bromination and KOH mediated anionic ring closure. GP2A, 2010, Rouen. 3. Application à la synthèse de ligands des récepteurs 5-HT4. Journée thématique Crunch « Organométalliques et Hétérocycles », 2009, Rouen. 2. Synthesis of substituted phenanthridinones for the development of new 5-HT4 receptors agonists. GP2A, 2009, Dublin, Ireland. 1. Décarboxylation - reprotonation énantiosélective par organocatalyse. Préparation d’acides alkyl-hémimaloniques pour la synthèse de l’impéranène. Journées des Jeunes Chercheurs de l'Ouest – Société Française de Chimie (JJC-SFC), 2007, Caen. Poster presentations (selection) 8. Synthesis of Cryptophane-111 derivatives usable for hyperpolarized 129Xe MRI. Journées de Chimie Organique, 2013, Palaiseau. 7. Synthèse d’un nouveau cryptophane-111 hexa-fonctionnalisé. Vers de nouvelles biosondes pour l’imagerie IRM 129 Xe. Journées des Jeunes Chercheurs de la Société de Chimie Thérapeutique(JJC-SCT), 2013, Romainville. 6. Selective functionalization of indazole: a rapid access to aza-analogues of psilocine. GP2A, 2011, Cork, Ireland. 5. Synthèse et évaluation biologique de nouveaux ligands des récepteurs 5-HT4. JJC-SCT, 2010, Paris 4. Synthèse de phénanthridinones substituées par cyclisation anionique. JJC-SCT, 2009, Paris. 3. Efficient synthesis of substituted phenanthridin-6(5H)-ones. Application to the development of new 5-HT4 receptor ligands. Rencontres chimie-biologie-santé, 2009, Rouen. 2. Study of KOH mediated anionic ring closure for the synthesis of substituted phenanthridinones. Application to the synthesis of thiophene analogues. Journée de l’Ecole Doctorale Normande Biologie Intègrative, Santé et Environnement, 2008, Le Havre. 1. Synthesis of substituted phenanthridinones by a KOH-mediated anionic ring closure. ANORCQ IX, 2008, Le Havre. Skills -Languages: french, english and scholar spanish. -Organic synthesis (multistep synthesis, fluorine chemistry, radiolabelling), heterocyclic and organometallic chemistry (pallado-catalyzed cross-coupling and C-H activation, ortho-lithiation, synthesis of boronic species, microwave reactions), medicinal chemistry (serotoninergic receptors, Alzheimer disease), supramolecular chemistry (cryptophane), imagery (Xe MRI, PET imagery). -Analytical skills: NMR (1H, 13C, 19F, 2D HH & CH, 129Xe), LC-MS, MS, HPLC, IR. -Computer technology: Windows Office and other usual softwares, SciFinder, Reaxys, Isis Draw, ChemBio Draw. Interests Culture: movies, novels, concerts and music, travels. Sports: badminton, jogging, swimming.