Raphaël Frédérick, PhD HOME OFFICE 33, allée de la Croix d’Al Faux B-5530 Godinne Belgium Phone: +32 (0) 81 22 20 15 (Private) +32 (0) 479 73 93 42 (Cell) E-mail: [email protected] Marital status: married Spouse’s name: Charlier Caroline Children: Frédérick Lucas (26/09/04) Frédérick Chloé (05/03/08) Frédérick Robin (25/03/2010) Nationality: Belgian Date of birth: 03-08-1978 Université Catholique de Louvain (UCL) Louvain Drug Research Institute (LDRI) Medicinal Chemistry Research Group (CMFA) Avenue Mounier 73 B-1200 Bruxelles Phone: +32 (0) 2 764 73 41 E-mail: [email protected] Educational, professional and teaching experiences 2013 - Professor, Chercheur Qualifié honoraire, CMFA group, Louvain Drug Research Institute (LDRI), Université Catholique de Louvain (UCL), Belgium 2011-2013 FRS-FNRS Research Associate; NAmur Medicine & Drug Innovation Centre (NAMEDIC), University of Namur, Belgium 2010-2013 Lecturer, University of Namur, Belgium 2007-2011 FRS-FNRS Postdoctoral Researcher; Laboratory of Structural and Biological Chemistry (Supervisor: Prof. Johan Wouters) and Department of Pharmacy (Supervisor: Prof. Bernard Masereel), University of Namur, Belgium. 2006-2007 Post-Doc Stay as Research Chemist at the Auckland Cancer Society Research Center (Supervisor: Prof. William A. Denny), University of Auckland, New Zealand 2001-2006 PhD in Pharmaceutical Sciences, Department of Pharmacy (Supervisor: Prof. Bernard Masereel), University of Namur, Belgium. 2001-2002 Master in Drug Design, Institut de Chimie Pharmaceutique Albert Lespagnol - ICPAL, University of Lille2, France. 2000-2001 Assistant, Laboratory of Molecular and Structural Chemistry (Supervisor: Prof. François Durant), University of Namur, Belgium. 1996-2000 A four-year-degree in Chemistry at the University of Namur, Belgium. 1 23/01/2014 Professional Societies - Société Royale de Chimie (SRC), Medicinal Chemistry section, member - Société de Chimie Thérapeutique (SCT), France, member - European Federation of Medicinal Chemistry (EFMC), member of the communication team - Télévie, member of the communication team Expert for funding Association - Agence Nationale de la Recherche - ANR (France) Referee for Scientific Journals - Journal of Medicinal Chemistry - Journal of Chemical Information and Modeling - Bioorganic and Medicinal Chemistry - Bioorganic and Medicinal Chemistry Letters - European Journal of Medicinal Chemistry - Medicinal Chemistry Communications - International Journal of Molecular Sciences Grants and Awards - 2013, UCL-FSR Crédit d’installation jeune académique - 2012, FUNDP-CERUNA Institutional Grant - 2011, FRS-FNRS Research Associate - 2007, FRS-FNRS Postdoctoral Researcher - 2006, Johnson and Johnson Pharmaceutical Research and Development Award for Young Medicinal Chemists (Dr. Paul Janssen award) - 2001, UCB award for the best poster communication Patents 1. “Novel TDO inhibitors” B. Van den Eynde, P. Larrieu, L. Pilotte, V. Stroobant, E. Dolusic, L. Moineaux, R. Frédérick, J. Wouters, B. Masereel, 2. “B-carboline derivatives with cytostatic properties” B. Masereel, J. Wouters, R. Frédérick, J Reniers, R. Kiss, C. Bruyère 3. “Tetraline sulphonamide derivatives useful in the treatment of proliferative disorders” B. Masereel, C. Supuran, R. Frédérick 2 23/01/2014 Publications 1. Novel Pyrazolo[1,5-a]pyridines as PI3K Inhibitors: Variation of the Central Linker Group Kendall JD, Marshall A, Giddens A, Tsang KY, Boyd, M Frédérick R., Lill C, Lee WJ, Kolekar S, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle G, Baguley B, Flanagan J, Denny WA and Shepherd P Med Chem Comm , 2014 5(1) 41-46 (Impact factor : 2.72) 2. Indoleamine 2,3-dioxygenase inhibitors: a patent review (2008 - 2012). Dolušić E, Frédérick R. Expert Opinion on Therapeutic Patent 2013, 23(10), 1367-1381 (Impact factor : 3.52) 3. Indoleamine 2,3-dioxygenase inhibitory activity of derivatives of marine alkaloid tsitsikammamine A Dolušić E., Larrieu P., Meinguet C., Colette D., Rives A., Blanc S., Ferain T., Pilotte L., Stroobant V., Wouters J, Van den Eynde B, Masereel B, Delfourne E, Frédérick R Bioorganic and Medicinal Chemistry Letters, 2013, 23(1), 47-54 (Impact Factor : 2.53) 4. New selective carbonic anhydrase IX inhibitors: Synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides Rogez-Florent T, Meignan S, Foulon C, Six P, Gros A, Bal-Mahieu C, Supuran CT, Scozzafava A, Frédérick R, Masereel B, Depreux P, Lansiaux A, Goossens JF, Gluszok S, Goossens L. Bioorganic and Medicinal Chemistry, 2013, 21(6):1451-64 (Impact Factor : 2.53) 5. Computational tools for in silico fragment-based drug design Mortier J., Rakers C., Frédérick R., Wolber G. Current topics in Medicinal Chemistry 2012, 12(17):1935-43 (Impact Factor : 4.17) 6. Novel trisubstituted harmine derivatives with original in vitro anticancer activity Frédérick R, Bruyère C, Vancraeynest C, Reniers J, Meinguet C, Pochet L, Backlund A, Masereel B, Kiss R, Wouters J. Journal of Medicinal Chemistry 2012 55(14):6489-501 (Impact Factor 4.89) 7. Synthesis, crystal structures and electronic properties of isomers of chloro-pyridinylvinyl-1Hindoles. Moineaux L, Laurent S, Reniers J, Dolušić E, Galleni M, Frère JM, Masereel B, Frédérick R, Wouters J. European Journal of Medicinal Chemistry 2012 54:95-102 (Impact Factor : 3.26) 8. Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase Pilotte L, Larrieu P, Stroobant V, Colau D, Dolusic E, Frédérick R, De Plaen E, Uyttenhove C, Wouters J, Masereel B, Van den Eynde B Proceedings of the National Academy of Sciences USA (2012), 109(7):2497-502 (Impact Factor : 9.77) 9. Discovery of pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors. Kendall JD, O'Connor PD, Marshall AJ, Frédérick R, Marshall ES, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR Bioorganic and Medicinal Chemistry (2012) 20(1), 69-85. (Impact Factor : 3.05) 10. Novel pyrazolo[1,5-a]pyridines as p110α-selective PI3 kinase inhibitors: Exploring the benzenesulfonohydrazide SAR Kendall JD, Giddens AC, Tsang KY, Frédérick R, Marshall ES, Singh R, Lill CL, Lee WJ, Kolekar S, Chao M, Malik A, Yu S, Chaussade C, Buchanan C, Rewcastle GW, Baguley BC, Flanagan JU, Jamieson SM, Denny WA, Shepherd PR. Bioorganic and Medicinal Chemistry (2012) 20(1), 58-68 (Impact Factor : 3.05) 3 23/01/2014 11. Synthesis and inhibition study of monoamine oxidase, indoleamine 2,3-dioxygenase and tryptophan 2,3-dioxygenase by 3,8-substituted 5H-indeno[1,2-c]pyridazin-5-one derivatives. Reniers J, Meinguet C, Moineaux L, Masereel B, Vincent SP, Frédérick R, Wouters J. European Journal of Medicinal Chemistry (2011) 46(12), 6104-6111 (Impact Factor : 3.26) 12. Synthesis and biological evaluation of novel analogues of the pan Class I phosphatidylinositol 3-kinase (PI3K) inhibitor 2-(difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1Hbenzimidazole (ZSTK474). Rewcastle GW, Gamage SA, Flanagan JU, Frédérick R, Denny WA, Baguley BC, Kestell P, Singh R, Kendall JD, Marshall ES, Lill CL, Lee WJ, Kolekar S, Buchanan CM, Jamieson SM, Shepherd PR. Journal of Medicinal Chemistry. (2011) 54(20), 7105-7126 (Impact Factor 4.89) 13. Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators. Dolusić E, Larrieu P, Moineaux L, Stroobant V, Pilotte L, Colau D, Pochet L, Van den Eynde B, Masereel B, Wouters J, Frédérick R. Journal of Medicinal Chemistry. (2011) 54(15), 5320-5334 (Impact Factor 4.89) 14. Discovery and preliminary SARs of Keto-Indoles as Novel Indoleamine 2,3-Dioxygenase (IDO) Inhibitors. Dolušić E., Larrieu P., Blanc S., Sapunaric S., Pouyez J., Moineaux L., Colette D., Stroobant V., Pilotte L., Colau D., Ferain T., Fraser G., Galeni M., Frère J.-M., Masereel B., Van den Eynde B., Wouters J., and Frédérick R. European Journal of Medicinal Chemistry, (2011) 46, 3058-3065 (Impact Factor : 3.26) 15. Indol-2-yl Ethanones as Novel Indoleamine 2,3-Dioxygenase (IDO) Inhibitors. Dolušić E., Larrieu P., Blanc S., Sapunaric S., Norberg B.., Moineaux L., Colette D., Stroobant V., Pilotte L., Colau D., Ferain T., Fraser G., Galeni M., Frère J.-M., Masereel B., a Van den Eynde B., Wouters J., and Frédérick R. Bioorganic and Medicinal Chemistry (2011) 19, 1550-1561 (Impact Factor : 3.05) 16. -carbolines dericatives as potential monoamine oxidase inhibitors. Reniers J., Robert S., Frédérick R., Masereel B., Vincent S., Wouters J. Bioorganic and Medicinal Chemistry (2011) 19, 134-144 (Impact Factor : 3.05) 17. Design, solid-phase synthesis, and biological evaluation of novel 1,5-diarylpyrrole-3carboxamides as carbonic anhydrase IX inhibitors Gluszok S., Frédérick R., Foulon C., Klupsch F., Supuran C.T., Vullo D., Scozzafava A., Goossens J.-F., Masereel B., Depreux P., Goossens L. Bioorganic and Medicinal Chemistry (2010) 18, 7392-7401 (Impact Factor : 3.05) 18. NF-kappaB inducing kinase (NIK) inhibitors: Identification of new scaffolds using virtual screening. Mortier J., Masereel B., Remouchamps C., Ganefe C., Piette J. Frédérick R. Bioorganic and Medicinal Chemistry Letters (2010) 20, 4515-4520 (Impact Factor : 2.53) 19. Pyrazolo[4,3-c]isoquinolines as Potential Inhibitors of NFMortier J. & Frédérick R., Ganefe C., Remouchamps C., Talaga P., Pochet L., Wouters J., Piette J., Dejardin E., Masereel B. Biochemical Pharmacology (2010) 79, 1462-1472 (Impact Factor: 4.83) 20. Phosphoinositide-3-kinase (PI3K) inhibitors : Identification of new scaffolds using virtual screening Frédérick R., Mawson C., Kendall J.D., Chaussade C., Rewcastle G.W., Shepherd P.R., Denny W.A. Bioorganic and Medicinal Chemistry Letters (2009) 19(20), 5842-5847 (Impact Factor : 2.53) 4 23/01/2014 21. Ligand-based and structure-based virtual screening to identify carbonic anhydrase IX inhibitors Thiry A., Ledecq M., Cecchi A., Frédérick R., Dogné J.-M., Supuran C., Wouters J., Masereel B. Bioorganic and Medicinal Chemistry Letters 17(2), 553-557 (2009) (Impact Factor : 2.53) 22. Molecular Modeling Approaches to the Design and Discovery of New Drugs: The Example of Phosphoinositide-3-Kinases (PI3Ks) Frédérick R., Denny W.A. Chimie Nouvelle 26(99), 8-14 (2008) (Impact Factor : NA) 23. Phosphoinositide-3-kinases (PI3Ks): combined comparative modelling and 3D-QSAR to rationalize the inhibition of p110alpha. Frédérick R., Denny W. Journal of Chemical Information and Modelling, 48(3), 629-638 (2008) (Impact Factor : 3.88) 24. Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors. Kendall J., Rewcastle G., Frédérick R., Mawson C., Denny W., Marschall E., Baguley B., Chaussade C., Jackson S., Shepherd, P. Bioorganic and Medicinal Chemistry Letters, 15, 7677-7687 (2007) (Impact Factor : 2.53) 25. Mechanism-Based Thrombin Inhibitors: Design, Synthesis, and Molecular Docking of a New Selective 2-Oxo-2H-1-benzopyran Derivative. Frédérick R., Robert S., Charlier C., Wouters J., Masereel B., Pochet, L. Journal of Medicinal Chemistry, 50, 3645-3650 (2007) (Impact Factor : 4.89) 26. Synthesis, structural reassignment and biological activity of type B MAO inhibitors based on the 5H-indeno-[1,2-c]pyridazin-5-one core. Frédérick R., Dumont W., Ooms F., Aschenbach L., Van der Schyf C., Castagnoli N., Wouters J. Krief A. Journal of Medicinal Chemistry, 49, 3743-3747 (2006) (Impact Factor : 4.89) 27. Investigation of mechanism-based thrombin inhibitors: implications of a highly conserved water molecule for the binding of coumarins within the S pocket. Frédérick R., Charlier C., Robert S., Wouters J., Masereel B., Pochet L. Bioorganic and Medicinal Chemistry Letters, 16, 2017-2021(2006) (Impact Factor : 2.53) 28. 3,6-disubstituted coumarins as mechanism-based inhibitors of Thrombin and Factor Xa, Frédérick R., Robert S., Charlier C., De Ruyck J., Wouters J., Pirotte B., Masereel B., Pochet L. Journal of Medicinal Chemistry, 48, 7592-7603 (2005) (Impact Factor : 4.89) 29. (E)-8-(3-Chlorostyryl)-1,3,7-trimethylxanthine, a caffeine derivative acting as antagonist of adenosine A2A receptors and as inhibitor of MAO-B, Frédérick R., Ooms F., Castagnoli N., Petzer J., Feng J.-F., Schwarzschild M.A., Van Der Schyf C., Wouters J. Acta crystallographica. Section C: Crystal structure communications, C61, o531-o532 (2005). (Impact Factor : 0.56) 30. Modulators of the coagulation cascade: Focus and Recent Advances in Inhibitors of Tissue Factor, Factor VIIa and their complex, Frédérick R., Pochet L., Charlier C., Masereel B. Current Medicinal Chemistry, 12, 397-417 (2005). (Impact Factor : 4.82) 31. Three 5H-indeno[1,2-c]pyridazin-5-one derivatives, potent type-B monoamine oxidase inhibitors, Frédérick R., Norberg B., Durant F., Ooms F., Wouters J. Acta crystallographica. Section C: Crystal structure communications, C60, o623-o626 (2004). (Impact Factor : 0.56) 5 23/01/2014 32. Coumarin and Isocoumarin as Serine Protease Inhibitors, Pochet L., Frédérick R., Masereel B. Current Pharmaceutical Design, 10, 3781-3796 (2004). (Impact Factor : 4.40) 33. Rational approaches towards reversible inhibition of type B monoamine oxidase: design and evaluation of a novel 5H-indeno[1,2-c]pyridazin-5-one derivative, Ooms F., Frédérick R., Durant F., Petzer J., Castagnoli N., Van Der Schyf C., Wouters J. Bioorganic and medicinal chemistry letters, 13, 69-73 (2003). (Impact Factor : 2.53) 34. Investigation of the inhibition mechanism of coumarins on chymotrypsin by mass spectrometry, Pochet L., Dieu M., Frédérick R., Murray A-M., Kempen I., Pirotte B., Masereel B. Tetrahedron, 59, 4557-4561 (2003). (Impact Factor : 2.89) Training of undergraduate students 2010 Mr Constant Manuel 2010 Mrs Modaffari Sara 2011 Mr Legrand Pierre 2012 Mrs Vanlemmputten Justine 2012 Mrs Bouchat Sandy 2013 Mrs Dochez Sarah 2013 Mrs Piedeleu Audrey 2013 Mrs Geneviève Masse Training of graduate students 2007-2011 Dr. Mortier Jérémie 2008-2012 Dr Moineaux Laurence 2013-2019 Mrs Alice Ameryckx Training of Postgraduate students 2013- Dr Serra Silvia 6 23/01/2014
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