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ID: ALA4339229

Journal: ACS Med Chem Lett

Title: Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia.

Authors: Quaglio D, Zhdanovskaya N, Tobajas G, Cuartas V, Balducci S, Christodoulou MS, Fabrizi G, Gargantilla M, Priego EM, Carmona Pestaña Á, Passarella D, Screpanti I, Botta B, Palermo R, Mori M, Ghirga F, Pérez-Pérez MJ.

Abstract: 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.

CiteXplore: 30996810

DOI: 10.1021/acsmedchemlett.8b00608