Research in Drug Development (RD3)

Microbiology, Bioorganic and Macromolecular Chemistry

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Research 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