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Optimization of the clofazimine structure leads to a highly water-soluble C3-aminopyridinyl riminophenazine endowed with improved anti-Wnt and anti-cancer activity in vitro and in vivo Koval, Alexey; Bassanini, Ivan; xu, Jiabin; Tonelli, Michele; ... Katanaev, Vladimir 2021
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Aglycone Ebselen and β-D-xyloside primed glycosaminoglycans co-contribute to Ebselen β-D-xyloside-induced cytotoxicity Tang, Yang; Zhang, Siqi; Chang, Yajing; Fan, Dacheng; ... Jiang, Tao 2018
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Cell-based multi-substrate assay coupled to UHPLC-ESI-MS/MS for a quick identification of class-specific HDAC inhibitors Zwick, Vincent; Simoes Avello, Claudia; Cuendet, Muriel 2016
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Biphenyl-4-yl-acrylohydroxamic acids: Identification of a novel indolyl-substituted HDAC inhibitor with antitumor activity Cincinelli, Raffaella; Zwick, Vincent; Musso, Loana; Zuco, Valentina; ... Dallavalle, Sabrina 2016
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Synthesis and evaluation of novel serotonin 4 receptor radiotracers for single photon emission computed tomography Lalut, Julien; Tournier, Benjamin; Cailly, Thomas; Lecoutey, Cédric; ... Rochais, Christophe 2016
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In silico driven design and synthesis of rhodanine derivatives as novel antibacterials targeting the enoyl reductase InhA Slepikas, Liudas; Chiriano, Gianpaolo; Perozzo, Remo; Tardy, Sébastien; ... Scapozza, Leonardo 2016
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Inhibition of Plasmodium falciparum Hsp90 Contributes to the Antimalarial Activities of Aminoalcohol-carbazoles Wang, Tai; Mäser, Pascal; Picard, Didier 2016
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Design of a serotonin 4 receptor radiotracer with decreased lipophilicity for single photon emission computed tomography Fresneau, Nathalie; Dumas, Noe; Tournier, Benjamin; Fossey, Christine; ... Fabis, Frédéric 2015
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Differences in Conformational Dynamics between Plasmodium falciparum and Human Hsp90 Orthologues Enable the Structure-Based Discovery of Pathogen-Selective Inhibitors Wang, Tai; Bisson, William Henry; Mäser, Pascal; Scapozza, Leonardo; Picard, Didier 2014
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Synthesis and structure-affinity relationships of selective high-affinity 5-HT(4) receptor antagonists: application to the design of new potential single photon emission computed tomography tracers Dubost, Emmanuelle; Dumas, Noe; Fossey, Christine; Magnelli, Rosa; ... Fabis, Frederic 2012
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Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors Leproult, Emeline; Barluenga, Sofia; Moras, Dino; Wurtz, Jean-Marie; Winssinger, Nicolas 2011
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Synthesis and characterization of a iodine-125-labeled pyrrolo[1,2-a]thieno[3,2-e]pyrazine and evaluation as a potential 5-HT4R SPECT tracer Cailly, Thomas; Dumas, Noe; Millet, Philippe; Lemaitre, Stephane; ... Rault, Sylvain 2010
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Discovery of a novel class of potent coumarin monoamine oxidase B inhibitors Pisani, Leonardo; Muncipinto, Giovanni; Miscioscia, Teresa Fabiola; Nicolotti, Orazio; ... Carotti, Angelo 2009
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Lipophilicity of basic drugs measured by hydrophilic interaction chromatography Bard, Bruno; Carrupt, Pierre-Alain; Martel, Sophie 2009
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Edaravone derivatives containing NO-donor functions Chegaev, Konstantin; Cena, Clara; Giorgis, Marta; Rolando, Barbara; ... Gasco, Alberto 2009
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Development of an in-capillary approach to nanoscale automated in vitro cytochromes p450 assays Nicoli, Raul; Curcio, Raffaele; Rudaz, Serge; Veuthey, Jean-Luc 2009
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High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists Henchoz, Yveline; Guillarme, Davy; Rudaz, Serge; Veuthey, Jean-Luc; Carrupt, Pierre-Alain 2008
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Antimitotic and antiproliferative activities of chalcones: forward structure-activity relationship Boumendjel, Ahcène; Boccard, Julien; Carrupt, Pierre-Alain; Nicolle, Edwige; ... Dumontet, Charles 2008
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NO-donor COX-2 inhibitors. New nitrooxy-substituted 1,5-diarylimidazoles endowed with COX-2 inhibitory and vasodilator properties Chegaev, K.; Lazzarato, L.; Tosco, P.; Cena, C.; ... Gasco, Alberto 2007
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In silico and in vitro filters for the fast estimation of skin permeation and distribution of new chemical entities Ottaviani, G.; Martel, Sophie; Carrupt, Pierre-Alain 2007
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