Chalcones and chalcone-mimetic derivatives as Notch inhibitors in a model of T-cell Acute Lymphoblastic Leukemia

01 Pubblicazione su rivista
Quaglio Deborah, Zhdanovskaya Nadezda, Tobajas Gloria, Cuartas Viviana, Balducci Silvia, Christodoulou Michael S., Fabrizi Giancarlo, Gargantilla Marta, Priego Eva-María, CARMONA PESTAñA Alvaro, Passarella Daniele, Screpanti Isabella, Botta Bruno, Palermo Rocco, Mori Mattia, Ghirga Francesca, Pérez-Pérez María-Jesús
ISSN: 1948-5875

Based on hit-likeness and chemical diversity, a number of chalcones and chalcone-mimetic compounds were selected as putative Notch inhibitors. The evaluation of the antiproliferative effect combined with the inhibition of Notch1 expression in KOPTK1 cell line identified compound 18, featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent.

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