Schnekenburger, Michael Goffin, Eric Lee, Jin-Young Jang, Jun Young Mazumder, Aloran Ji, Seungwon Rogister, Bernard Bouider, Nafila Lefranc, Florence Miklos, Walter
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Published in
Journal of medicinal chemistry
A new series of N-aryl-N'-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)ureas bearing an alkoxycarbonylamino group at the 6-position were synthesized and examined as putative anticancer agents targeting sirtuins in glioma cells. On the basis of computational docking combined to in vitro sirtuin 1/2 inhibition assays, we selected compound 18 [R/S-N-...
Doering, Mandy Ba, Lalla A. Lilienthal, Nils Nicco, Carole Scherer, Christiane Abbas, Muhammad Ali Peer Zada, Abdul Coriat, Romain Burkholz, Torsten Wessjohann, Ludger
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Published in
Journal of Medicinal Chemistry
Many tumor cells exhibit a disturbed intracellular redox state resulting in higher levels of reactive oxygen species (ROS). As these contribute to tumor initiation and sustenance, catalytic redox agents combining significant activity with substrate specificity promise high activity and selectivity against oxidatively stressed malignant cells. We de...
Valente, Sergio Liu, Yiwei Schnekenburger, Michael Zwergel, Clemens Cosconati, Sandro Gros, Christina Tardugno, Maria Labella, Donatella Florean, Cristina Minden, Steven
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DNA methyltransferases (DNMTs) are important enzymes involved in epigenetic control of gene expression and represent valuable targets in cancer chemotherapy. A number of nucleoside DNMT inhibitors (DNMTi) have been studied in cancer, including in cancer stem cells, and two of them (azacytidine and decitabine) have been approved for treatment of mye...
Ebrahim, Weaam Aly, Amal H. Wray, Victor Mándi, Attila Marie-Hélène Teiten Francois Gaascht Barbora Orlikova Kassack, Matthias U. Lin, Wenhan Marc Diederich
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Published in
Journal of Medicinal Chemistry
Two new metabolites, embellicines A and B (1 and 2), were isolated from the EtOAc extract of the fungus Embellisia eureka, an endophyte of the Moroccan plant Cladanthus arabicus (Asteraceae). The structures of these new compounds were determined on the basis of extensive one- and two-dimensional NMR spectroscopy as well as by high-resolution mass s...
