Since 2013, my research activities have focused on medicinal chemistry. My activity is centered on the development of new therapeutic molecules. Pathologies of interest are parasitic diseases such as malaria (Plasmodiums), trypanosmiases (Chagas disease, sleeping sickness ... due to Trypanosomas) and leishmaniases (visceral and cutaneous due to Leishmanias). Thus, the synthesis of new derivatives for the treatment of these diseases are carried out. In addition, I’m also conducting research to elucidate the mechanisms of action of the new synthesized molecules, either in the laboratory or in collaboration. The new derivatives are also tested on different parasites by collaboration with BIOCIS for their antiparasitic activities (3 publications).
Since September 2015, I am also involved in a European project (JPIAMR) for the synthesis of carbapenemase inhibitors (NDM-1) directed against antibiotic-resistant bacterial strains (Gram-negative bacteria) (1 patent in preparation).
Finally, since January 2016, a new project has been set up on the development of anti-cancer agents by pharmacomodulation of natural molecules (Gambogic acid, Tagitinin C) in partnership with Pr G. Vo-Thanh (ICMMO, ECM). Two teams of biologists are involved in the project: one team in Vietnam and another in Korea (1 publication in preparation).
In-cell generation of anticancer phenanthridine through bioorthogonal cyclization: a paradigm in antitumor prodrug development. H. Maslah, C. Skarbek, C. Gourson, M.-A. Plamont, S. Pethe, L. Jullien, T. Le Saux, R. Labruère, Angew. Chem. Int. Ed., 2021, 60, 24043-24047
Structural modification and biological activity studies of Tagitinin C and its derivatives. T. H. Au, C. Skarbek, S. Pethe, R. Labruère, J.-P. Baltaze, T. P. Hoa Nguyen, T. T. H. Vu, G. Vo-Thanh, Tetrahedron, 2021, 132248
Boronic acid/boronate prodrugs for cancer treatment: current status and perspectives. H. Maslah, S. Pethe, R. Labruère, Future Med. Chem., 2021, 13, 859-861
Anticancer boron-containing prodrugs responsive to oxidative stress from the tumor microenvironment. H. Maslah, C. Skarbek, S. Pethe, R. Labruère, Eur. J. Med. Chem., 2020, 112670
Spermine-NBD as fluorescent probe for studies of the polyamine transport system in Leishmania donovani. E. Jagu, S. Pomel, S. Pethe, J.-C. Cintrat, P. M. Loiseau, R. Labruère, Bioorg. Med. Chem. Lett., 2019, 29, 1710-1713
Synthesis and antikinetoplastid evaluation of bis(benzyl)spermidine derivatives. E. Jagu, S. Pomel, A. Diez-Martinez, E. Rascol, S. Pethe, P. M. Loiseau, R. Labruère, Eur. J. Med. Chem., 2018, 150, 655-666
Polyamine-based analogs and conjugates as antikinetoplastid agents. E. Jagu, S. Pomel, S. Pethe, P. M. Loiseau, R. Labruère, Eur. J. Med. Chem., 2017, 139, 982-1015
Synthesis and in vitro antikinetoplastid activity of polyamine-hydroxybenzotriazole conjugates. E. Jagu, S. Pomel, A. Diez-Martinez, F. Ramiandrasoa, R. Luise Krauth-Siegel, S. Pethe, C. Blonski, R. Labruère, P. M. Loiseau, Bioorg. Med. Chem., 2017, 25, 84-90
Design, synthesis and in vitro antikinetoplastid evaluation of N-acylated putrescine, spermidine and spermine derivatives. E. Jagu, R. Djilali, S. Pomel, F. Ramiandrasoa, S. Pethe, R. Labruère, P. M. Loiseau, C. Blonski, Bioorg. Med. Chem. Lett., 2015, 25, 207-209