Moderately lipophilic 2-(Het)aryl-6-dithioacetals, 2-phenyl-1,4-benzodioxane-6-dithioacetals and 2-phenylbenzofuran-5-dithioacetals: Synthesis and primary evaluation as potential antidiabetic AMPK-activators

Autor: Veronica Lepechkin-Zilbermintz, Daniel Bareket, Virginie Gonnord, Alexandre Steffen, Christophe Morice, Mathieu Michaut, Anna Munder, Edward E. Korshin, Jean-Marie Contreras, Erol Cerasi, Shlomo Sasson, Arie Gruzman

Publikováno v: Bioorganic & Medicinal Chemistry. 87:117303

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::90fa71b45153506dcca96edbee318c50
https://doi.org/10.1016/j.bmc.2023.117303

N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK

Autor: Stefano Sainas, Jean-Marie Contreras, Alessandro Barge, Salam Al-Karadaghi, Alex Ducime, Agnese Chiara Pippione, Marco Lucio Lolli, Antonella Federico, Elisa Lupino, Michael Kubbutat, Christophe Morice, Marco Piccinini, Donatella Boschi

Publikováno v: MedChemComm. 9:963-968

NF-κB-inducing kinase (NIK), an oncogenic drug target that is associated with various cancers, is a central signalling component of the non-canonical pathway. A blind screening process, which established that amino pyrazole related scaffolds have an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c9c8d94a1160855842ae6a928f29d0c
https://doi.org/10.1039/c8md00068a

4-Hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide: a novel inhibitor of the canonical NF-κB cascade

Autor: Alex Ducime, Agnese Chiara Pippione, Marco Piccinini, Salam Al-Karadaghi, Marco Lucio Lolli, Christophe Morice, Donatella Boschi, Elisa Lupino, Antonella Federico, Stefano Sainas, Jean-Marie Contreras, Alessandro Barge, Michael Kubbutat

Publikováno v: MedChemComm. 8:1850-1855

The NF-κB signaling pathway is a validated oncological target. Here, we applied scaffold hopping to IMD-0354, a presumed IKKβ inhibitor, and identified 4-hydroxy-N-[3,5-bis(trifluoromethyl)phenyl]-1,2,5-thiadiazole-3-carboxamide (4) as a nM-inhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc032ac0d2a2596a02501de0edb20aac
https://doi.org/10.1039/c7md00278e

Approved drugs screening against the nsP1 capping enzyme of Venezuelan equine encephalitis virus using an immuno-based assay

Autor: Bruno Canard, Ana Sofia Ferreira Ramos, Jean-Marie Contreras, Changqing Li, Marie-Louise Jung, Christophe Morice, Gilles Querat, Etienne Decroly, María-Jesús Pérez Pérez, Bruno Coutard, Alba Gigante, Cécilia Eydoux, Jean-Claude Guillemot

Publikováno v: Antiviral Research
Antiviral Research, Elsevier Masson, 2019, 163, pp.59-69. ⟨10.1016/j.antiviral.2019.01.003⟩
Antiviral Research, 2019, 163, pp.59-69. ⟨10.1016/j.antiviral.2019.01.003⟩
Antiviral Research, Elsevier Masson, 2019, 163, pp.59-69. 〈10.1016/j.antiviral.2019.01.003〉
Hyper Article en Ligne
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Alphaviruses such as the Venezuelan equine encephalitis virus (VEEV) are important human emerging pathogens transmitted by mosquitoes. They possess a unique viral mRNA capping mechanism catalyzed by the viral non-structural protein nsP1, which is ess

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3bbf70c72e0ca4161f1fb0323e2553d
http://hdl.handle.net/10261/177171

Discovery, Structure-Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain-Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4

Autor: Millan Ortiz, Baptiste Manteau, Rachel Rudigier, Stephan Schann, Gaël Hédou, Nadia Brugger, Laurène Deshons, François Conquet, Edith Steinberg, Vincent Pomel, Luc Baron, Delphine Charvin, Delphine Thiarc, Danielle Graham, Sophie Scheffler, Stanislas Mayer, Mélanie Frauli, Bruno Giethlen, Christophe Morice

Publikováno v: Journal of medicinal chemistry. 60(20)

The metabotropic glutamate receptor 4 (mGluR4) is an emerging target for the treatment of Parkinson's disease (PD). However, since the discovery of its therapeutic potential, no ligand has been successfully developed enough to be tested in the clinic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bbc29e55d23c1e6109bea421cb14f221
https://pubmed.ncbi.nlm.nih.gov/28902994