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SCIENCE > Publications

2010

Antonio Garofalo, Laurence Goossens, Amélie Lemoine, Amaury Farce, Yannick Arlot and Patrick Depreux. Quinazoline-urea, new protein kinase inhibitors in treatment of prostate cancer; 2010; 25(2): 158-170
E. Lipka, M.P. Vaccher, J.P. Bonte, C. Vaccher. Chiral capillary electrophoresis with highly sulfated cyclodextrins. Resolution of benzoxazolinone aminoalcohols and aminoketon precursors, potential adrenergic ligands; 2010, acceptée
C. Reynes, H. Host, A.C. Camproux, G.Laconde, F. Leroux, A. Mazars, B. Deprez, R. Fahraeus, B.O. Villoutreix & O. Sperandio. Designing Focused Chemical Libraries Enriched in Protein-Protein Interaction Inhibitors using Machine-Learning Methods; 2010, 6(3): e1000695.
S. Malaquin, M. Jida, J.C. Gesquière, R. Deprez-Poulain, B. Deprez, G. Laconde. Ugi reaction for the synthesis of 4-aminopiperidines-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil; 2010, 51_2983
F. Siepmann, K. Eckart, A. Maschke, K. Kolter, J. Siepmann. Modeling drug release from PVAc/PVP matrix tablets; 2010 submitted
S. Malaquin, M. Jida, R. Deprez-Poulain, G. Laconde, B. Deprez. Tetrahedron Lett. Synthesis of 5- and 6-membered lactams via Ugi reaction under solvent-free microwave assistance; 2010 submitted
E. Lipka, M. Folly-Klan, M.P. Vaccher, J. charton, J.P. Bonte, C. Vaccher. Determination of pKa values of benzimidazole derivatives, potent AMPK activators, by capillary electrophoresis; 2010 soumise
Q.W. Yang; M.P. Flament, F. Siepmann, V. Busignies, B. Leclerc, C. Herry, P. Tchoreloff, J. Siepmann. Curing of aqueous polymeric film coatings: Importance of the coating level and type of plasticizer; 2010 in press
M. Jida, R. Deprez-Poulain, S. Malaquin, P. Roussel, F. Agbossou-Niedercorn, B. Deprez, G. Laconde. Solvent-free microwave-assisted Meyers’ lactamization; 2010 in press
E. Lipka, C. Danel, S. Yous, J.P. Bonte, C. Vaccher. Dual cyclodextrin system in capillary electrophoresis for direct separation of the four stereoisomers of agonist and antagonist melatoninergic ligands; 2010 31, acceptée
AC. Carbodery, M. Toussaint, J.P. Bonte, P. Melnyk, C. Vaccher, C. Foulon. Separation of Tic-hydantoin enantiomers, potent sigma-1 agonist, by high performance liquid chromatography and capillary electrophoresis; 2010 acceptée

2009

M. Flipo, J. Charton, J. A. Hocine, S. Dassonneville, B. Deprez, R. Deprez-Poulain. Hydroxamates: Relationships between structure and plasma-stability; 2009, 52, (21), 6790-6802
D. Dumoulin, S. Lebrun, E. Deniau, A. Couture, P. Grandclaudon. First asymmetric synthesis of (un)saturated 1-alkyl benzo[c]azepin-3-ones. Extension to the corresponding benzazepines; 2009, 3741-3752
E. Lipka, J. Charton, M.P. Vaccher, M. Folly-Klan, C. Vaccher. Enantioseparation of chiral benzimidazole derivatives by electrokinetic chromatography using sulfated cyclodextrins; 2009, 32(11), 1907-1915
C. Foulon, J. Tedou, T. Queruau Lamerie, C. Vaccher, J.P. Bonte, J.F. Goossens. Assessment of the complexation degree of camptothecin derivatives and cyclodextrins using spectroscopic and separatives methodologies; 2009, 20, 2482-2489
D. Dumoulin, S. Lebrun, A. Couture, E. Deniau, P. Grandclaudon. Asymmetric synthesis of 3- or 4-alkyl or arylbenzo[c]azepines; 2009, 20, 1903–1911
J. Charton, R. Deprez-Poulain, N. Hennuyer, A. Tailleux, B. Staels, B. Deprez, Novel non-carboxylic acid retinoids: 1,2,4-Oxadiazol-5-one derivatives; 2009, 19, (2), 489-492
N. Willand, B. Dirié, X. Carette, P. Bifani, A. Singhal, M. Desroses, F. Leroux, R. Déprez-Poulain, F. Frénois, M. Aumercier, C. Locht, V. Villeret, B. Déprez, A. Baulard. Synthetic EthR inhibitors boost anti-tuberculous activity of ethionamide; 2009, 15, 537-544
E. Lipka, C. Vaccher, J.P. Bonte, C. Foulon. Capillary Electrophoresis and High Performance Liquid Chromatography for Chiral Separation of Four Piperidinic Benzoxazolinone Compounds; 2009 69, 903-909
E. Lipka, C. Vaccher, J.P. Bonte. Enantiomeric resolution of benzoxazolinone amino alcohols, potential adrenergic ligands, by LC and CE; 2009 69, 465-472
C. Danel, N. Azaroual, D. Lannoy, A. Brunel, P. Odou, B. Decaudin, G. Vermeersch, J.P. Bonte, C. Vaccher Chiral stability of the 9-hydroxyrisperidone. Kinetics and mechanism of racemization; 2009 20(10), 1125-1131
S. Muschert, F. Siepmann, B. Leclercq, B. Carlin, J. Siepmann. Prediction of drug release from ethylcellulose coated pellets; 2009
S. Muschert, F. Siepmann, B. Leclercq, B. Carlin, J. Siepmann. Drug release mechanisms from ethylcellulose: PVA-PEG graft copolymer coated pellets; 2009
S. Muschert, F. Siepmann, Y. Cuppok, B. Leclercq, B. Carlin, J. Siepmann. Improved long term stability of aqueous ethylcellulose film coatings: Importance of the type of drug and starter core; 2009
D. Klose, N. Azaroual, F. Siepmann, G. Vermeersch, J. Siepmann. Towards more realistic in vitro release measurement techniques for biodegradable microparticles; 2009
D. Klose, M. Laprais, V. Leroux, F. Siepmann, B. Deprez, R. Bordet, J. Siepmann. Fenofibrate-loaded PLGA microparticles: Effects on ischemic stroke; 2009
Y. Karrout, C. Neut, D. Wils, F. Siepmann, L. Deremaux, L. Dubreuil, P. Desreumaux, J. Siepmann. Colon targeting with bacteria-sensitive films adapted to the disease state; 2009
L. Ho, Y. Cuppok, S. Muschert, K.C. Gordon, M. Pepper, Y. Shen, F. Siepmann, J. Siepmann, P.F. Taday, T. Rades. Effects of film coating thickness and drug layer uniformity on in-vitro drug release from sustained-release coated pellets: A case study using terahertz pulsed imaging; 2009
B. Glaessl, F. Siepmann, I. Tucker, J. Siepmann, T. Rades. Characterization of quaternary polymethacrylate films containing tartaric acid, metoprolol free base or metoprolol tartrate; 2009
Catherine Foulon, Josette Tedou, Thomas Queruau Lamerie, Jean-Paul Bonte, Claude Vaccher, Jean-Francois Goossens. Assessment of the complexation degree of camptothecin derivatives and cyclodextrins using spectroscopic and separative methodologies; 2009
Anne Thiry, Aurélie Delayen, Laurence Goossens, Raymond Houssin, Marie Ledecq, Aurélie Frankart, Jean-Michel Dogné, Johan Wouters, Claudiu T. Supuran, Jean-Pierre Hénichart, Bernard Masereel. Synthesis and biological evaluation of a new family of anti-benzylanilinosulfonamides as CA IX inhibitors; 2009

2008

J. Charton, L. Charruault, R. Deprez-Poulain & B. Deprez. Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds; 2008b, 11(4): 294-303
J. Charton, F. Leroux, S. Delaroche, V. Landry, B.P. Deprez & R.F. Deprez-Poulain. Synthesis of a Library of 200-Member Squaric Acid N-Hydroxylamide Amides; 2008a, 18(18): 4968-4971
B.O. Villoutreix, K. Bastard, O. Sperandio, R. Fahraeus, J.L. Poyet, F. Calvo, B. Deprez & M.A. Miteva. In silico-in vitro screening of protein-protein interactions: towards the next generation of therapeutics; 2008, 9(2): 103-122
T. Beghyn, R. Deprez-Poulain, N. Willand N, B. Folleas, B. Deprez. Natural compounds: Leads or ideas? Bioinspired molecules for drug discovery; 2008, 72, 1, 3-15
N. Cousaert, N. Willand, J.C. Gesquiere, A. Tartar, B. Deprez & R. Deprez-Poulain. Original loading and Suzuki conditions for the solid-phase synthesis of biphenyltetrazoles. Application to the first solid-phase synthesis of irbesartan; 2008, 49: 2743-2747
J.F. Goossens, A.L. Villard, C. Perigaud, J.P. Bonte, C. Vaccher, C. Foulon. Chiral separation of nucleoside phosphoramidates diastereoisomers by high performance liquid chromatography and capillary electrophoresis; 2008 875, 288-295
C. Danel, N. Azaroual, A. Brunel, D. Lannoy, P. Odou, G. Vermeesch, C. Vaccher. Risperidone and 9-hydroxyrisperidone: study of the complexation with cyclodextrin-hosts using affinity capillary electrophoresis and 1H NMR; 2008 1205 (1), 185-193

2007

M. Flipo, T. Beghyn, V. Leroux, I. Florent, B.P. Deprez & R.F. Deprez-Poulain. Novel Selective Inhibitors of the Zinc Plasmodial Aminopeptidase PfA-M1 as Potential Antimalarial Agents; 2007, 50(6): 1322-1334
J. Charton, N. Cousaert, C. Bochu, N. Willand, B. Deprez & R. Deprez-Poulain. A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues; 2007, 48(8): 1479-1483.
R.F. Deprez-Poulain, J. Charton, V. Leroux & B.P. Deprez. Convenient synthesis of 4H-1,2,4-triazole-3-thiols using di-2-pyridylthionocarbonate; 2007, 48(46): 8157-8162.
N. Willand, B. Folléas, C. Boutillon, L. Verbraeken, J.C. Gesquiere, A. Tartar & B. Deprez. Efficient, Two-Step Synthesis Of N-Substituted Nortropinone Derivatives; 2007, 48(29): 5007-5011
T. Beghyn, C. Hounsou & B.P. Deprez. PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil; 2007, 17(3): 789-792
M. Flipo, T. Beghyn, J. Charton, V.A. Leroux, B.P. Deprez & R.F. Deprez-Poulain. A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening; 2007, 15(1): 63-76
E. Lipka, C. Danel, H. Orhan, J.P. Bonte, C. Vaccher. Chiral resolution of six melatoninergic ligands, by electrokinetic chromatography using highly sulfated cyclodextrins; 2007 28(21), 3915-3921
C. Danel, P. Chaminade, P. Odou, C. Barthelemy, D. Azarzar, J.P. Bonte, C. Vaccher. Enantioselective analysis of the antipsychotic 9-hydroxyrisperidone, main metabolite of risperidone, by chiral capillary electrokinetic chromatography using dual cyclodextrins; 2007 28(15), 2683-2692
C. Danel, P. Odou, C. Barthelemy, D. Azarzar, H. Robert, J.P. Bonte, C. Vaccher. Analytical and semipreparative enantioresolution of 9-hydroxyrisperidone, main metabolite of risperidone using high performance liquid chromatography and capillary zone electrophoresis. Validation and determination of enantiomeric purity; 2007 1163(1-2), 226-236
C. Foulon, N. Duhal, B. Lacroix-Callens, C. Vaccher, J.P. Bonte, J.F. Goossens. Determination of pKa values of benzoxa-, benzothia- and benzoselena-zolinone derivatives from mobility obtained by capillary electrophoresis. Comparison with potentiometric titration and spectroscopic data; 2007 31, 165-171
A. Lansiaux, S. Léonce, L. Kraus-Berthier, C. Bal, R. Mazinghien, M.H. David-Cordonnier, P. Hautefaye, G. Lavielle, C. Bailly, A. Pierré, J. Hickman. Novel camptothecin derivatives lacking the lactone function: potent inhibitors of topoisomerase I and promising antitumor drugs; 2007