Raphael Labruere
Dr Raphael Labruere, Associate Professor of Chemistry
After studying biochemistry/chemistry (Paris Descartes and Paris Diderot universities), he obtained his PhD in chemistry in December 2006 (organic and medicinal chemistry of antivascular azalignans under the supervision of Pr. S. Giorgi-Renault, University Paris Descartes, Faculty of Pharmacy). Then he moved to the U.S. as a postdoctoral researcher on a two-year contract (group of Prof. E. Turos; University of South Florida), where he developed polymeric nanoparticles as drug delivery vehicles. In October 2010, after a year as lecturer in therapeutic chemistry (chemoenzymatic synthesis; group of Prof. M. Vidal, University Paris Descartes, Faculty of Pharmacy), he then worked on kinetically tunable self-immolative spacers as optical syringe for biological applications (collaborative project between Institut Curie and Ecole normale supérieure-Paris under the supervision of Dr. F. Schmidt and Prof. L. Jullien). Appointed as Assistant Professor (Maître de Conférences) at University Paris-Sud in September 2013, he joined the « Equipe de Chimie Bioorganique et Bioinorganique », Institut de Chimie Moléculaire et des Matériaux d’Orsay (ICMMO, UMR 8182). His expertise covers heterocyclic synthesis and pharmacological evaluation of small molecules (drugs and prodrugs), and the synthesis and kinetic study of quinone methide-based self-immolative spacers.
Latest publications
Synthesis of 6-methylphenanthridines and evaluation against human papillomavirus-related endocervical adenocarcinoma (KB 3.1) cells. H. Maslah, C. Skarbek, R. Labruère, Phytochem. Lett., 2023, 54, 146-152
Re-designing environmentally persistent pharmaceutical pollutant through programmed inactivation: The case of methotrexate. A. Espinosa, E. Rascol, M. A. Flos, C. Skarbek, P. Lieben, E. Bannerman, A. D. Martinez, S. Pethe, P. Benoit, S. Nélieu, R. Labruère, Chemosphere, 2022, 306, 135616
Photodegradation of methotrexate in aqueous solution: degradation kinetics and identification of transformation products. A. Espinosa, S. Nélieu, P. Lieben, C. Skarbek, R. Labruère, P. Benoit, Environ. Sci. Pollut. Res., 2022, 29, 6060-6071
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, 92, 132248
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, 207, 112670
Anti–Methicillin-Resistant Staphylococcus aureus Nanoantibiotics. R. Labruère, A. J. Sona, E. Turos, Front. Pharmacol., 2019, 10, 01121
Arylboronate prodrugs of doxorubicin as promising chemotherapy for pancreatic cancer. C. Skarbek, S. Serra, H. Maslah, E. Rascol, R. Labruère, Bioorg. Chem., 2019, 91, 103158
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
A chemically-encoded timer for dual molecular delivery at tailored ranges and concentrations. S. Serra, A. Alouane, T. Le Saux, S. Huvelle, A. Alouane, R. Plasson, F. Schmidt, R. Labruère, Chem. Commun., 2018, 54, 6396-6399
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
Self-Immolative Spacers: Kinetic Aspects, Structure–Property Relationships, and Applications. A. Alouane, R. Labruère, T. Le Saux, F. Schmidt, L. Jullien, Angew. Chem. Intern. Ed., 2015, 54, 7492-7509
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