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François Dufrasne
Research in Drug Development (RD3)
Microbiology, Bioorganic and Macromolecular Chemistry
ContactResearch activities
His main research interests focus on the design and synthesis of organic or inorganic molecules having potential therapeutic applications in health.
He is especially involved in solving problems related to the finding of new hits as receptor agonists/antagonists or enzyme inhibitors in collaboration with other teams working on molecular docking and protein crystallization in the University.Further developments can be made in-house such as lead generation, toxicological testing and drug preformulation to achieve animal testing.
Top ten recent articles
Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure
Soubhye, J., Chikh Alard, I., Aldib, I., Prévost, M., Gelbcke, M., De Carvalho, A., Furtmüller, P. G., Obinger, C., Flemmig, J., Tadrent, S., Meyer, F., Rousseau, A., Neve, J., Mathieu, V., Zouaoui Boudjeltia, K., Dufrasne, F., & Van Antwerpen, P. (2017). Discovery of Novel Potent Reversible and Irreversible Myeloperoxidase Inhibitors Using Virtual Screening Procedure. Journal of medicinal chemistry, 60(15), 6563-6586. doi:10.1021/acs.jmedchem.7b00285
Resonant X-ray emission spectroscopy of platinum(ii) anticancer complexes.
Sá, J., Czapla-Masztafiak, J., Lipiec, E., Kayser, Y., Fernandes, D. L. A., Szlachetko, J., Dufrasne, F., & Berger, G. (2016). Resonant X-ray emission spectroscopy of platinum(ii) anticancer complexes. Analyst, 141(4), 1226-1232. doi:10.1039/c5an02490k
Insights into the structure-activity relationships of chiral 1,2-diaminophenylalkane platinum(II) anticancer derivatives.
Berger, G., Fusaro, L., Luhmer, M., Czapla-Masztafiak, J., Lipiec, E., Szlachetko, J., Kayser, Y., Fernandes, D. L. A., Sá, J., Dufrasne, F., & Bombard, S. (2015). Insights into the structure-activity relationships of chiral 1,2-diaminophenylalkane platinum(II) anticancer derivatives. JBIC. Journal of biological inorganic chemistry. doi:10.1007/s00775-015-1270-6
Synthesis and in vitro characterization of platinum(II) anticancer coordinates using FTIR spectroscopy and NCI COMPARE: A fast method for new compound discovery.
Berger, G., Leclercqz, H., Derenne, A., Gelbcke, M., Goormaghtigh, E., Neve, J., Mathieu, V., & Dufrasne, F. (2014). Synthesis and in vitro characterization of platinum(II) anticancer coordinates using FTIR spectroscopy and NCI COMPARE: A fast method for new compound discovery. Bioorganic & medicinal chemistry, 22(13), 3527-3536. doi:10.1016/j.bmc.2014.04.017
The antiapoptotic effect of remifentanil on the immature mouse brain: An ex vivo study
Tourrel, F., Laudenbach, V., Gonzalez, B. J., Jégou, S., De Lendeu, P. K., Abily-Donval, L., Chollat, C., Marret, S., Dufrasne, F., Compagnon, P., Ramdani, Y., & Dureuil, B. (2014). The antiapoptotic effect of remifentanil on the immature mouse brain: An ex vivo study. Anesthesia and analgesia, 118(5), 1041-1051. doi:10.1213/ANE.0000000000000159
Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors.
Soubhye, J., Aldib, I., Elfving, B., Gelbcke, M., Furtmüller, P. G., Podrecca, M., Conotte, R., Colet, J.-M., Rousseau, A., Reye, F., Sarakbi, A., Vanhaeverbeek, M., Kauffmann, J.-M., Obinger, C., Neve, J., Prévost, M., Zouaoui Boudjeltia, K., Dufrasne, F., & Van Antwerpen, P. (2013). Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors. Journal of medicinal chemistry, 56(10), 3943-3958. doi:10.1021/jm4001538
Synthesis of 15N-labeled vicinal diamines through N-activated chiral aziridines: tools for the NMR study of platinum-based anticancer compounds
Berger, G., Gelbcke, M., Cauet, E., Luhmer, M., Neve, J., & Dufrasne, F. (2013). Synthesis of 15N-labeled vicinal diamines through N-activated chiral aziridines: tools for the NMR study of platinum-based anticancer compounds. Tetrahedron letters, 54(6), 545-548. doi:10.1016/j.tetlet.2012.11.079
Evaluation of new scaffolds of myeloperoxidase inhibitors by rational design combined with high-throughput virtual screening
Aldib, I., Soubhye, J., Zouaoui Boudjeltia, K., Vanhaeverbeek, M., Rousseau, A., Furtmüller, P. G., Obinger, C., Dufrasne, F., Neve, J., Van Antwerpen, P., & Prévost, M. (2012). Evaluation of new scaffolds of myeloperoxidase inhibitors by rational design combined with high-throughput virtual screening. Journal of medicinal chemistry, 55(16), 7208-7218. doi:10.1021/jm3007245
Structure-based design, synthesis, and pharmacological evaluation of 3-(Aminoalkyl)-5-fluoroindoles as myeloperoxidase inhibitors.
Soubhye, J., Prévost, M., Van Antwerpen, P., Zouaoui Boudjeltia, K., Rousseau, A., Furtmüller, P. G., Obinger, C., Vanhaeverbeek, M., Ducobu, J., Neve, J., Gelbcke, M., & Dufrasne, F. (2010). Structure-based design, synthesis, and pharmacological evaluation of 3-(Aminoalkyl)-5-fluoroindoles as myeloperoxidase inhibitors. Journal of medicinal chemistry, 53(24), 8747-8759. doi:10.1021/jm1009988
The relation between stereochemistry and biological activity of platinum(II) complexes chelated with chiral diamine ligands: an intricate problem.
Dufrasne, F., & Galanski, M. (2007). The relation between stereochemistry and biological activity of platinum(II) complexes chelated with chiral diamine ligands: an intricate problem. Current pharmaceutical design, 13(27), 2781-2794. doi:10.2174/138161207781757060
Career
- Lecturer at the Faculty of Medicine and Pharmacy of the University of Mons (Belgium) (2007-).
- Lecturer at the Faculty of Medicine (ULB) for the Pharmed courses (2007-).
- Lecturer at the Faculty of Pharmacy of (ULB) (2006-).
- Assistant-professor at the Faculty of Pharmacy (ULB) (2002-2006)
- Assistant in the Laboratory of Organic Pharmaceutical Chemistry (Institute of Pharmacy, ULB) (1996-2002) .
- PhD in pharmaceutical sciences (Title: “Conception and synthesis of new stereoselective organic ligands of platinum(II)”), Institute of Pharmacy (ULB) (1996-2002).
- Diplome d’étude approfondie en sciences de la santé” at the Institute of Pharmacy (ULB) (2001).
- Pharmacist in (1990-1996) with “grande distinction” at the Institute of Pharmacy of the Université Libre de Bruxelles (ULB, Belgium).