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Title Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia
Authors Quaglio, Deborah , Zhdanovskaya, Nadezda , Tobajas, Gloria , Cuartas, Viviana , Balducci, Silvia , Christodoulou, Michael S. , Fabrizi, Giancarlo , Gargantilla, Marta , Priego, Eva-Maria , CARMONA PESTAÑA, ÁLVARO, Passarella, Daniele , Screpanti, Isabella , Botta, Bruno , Palermo, Rocco , Mori, Mattia , Ghirga, Francesca , Jesus Perez-Perez, Maria
External publication Si
Means ACS Med. Chem. Lett.
Scope Article
Nature Científica
JCR Quartile 2
SJR Quartile 1
JCR Impact 3.975
SJR Impact 1.158
Publication date 01/04/2019
ISI 000464767700043
DOI 10.1021/acsmedchemlett.8b00608
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 Notchl expression in KOPTK1 cell line identified compound 18, featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent.
Keywords Chalcone; tetrahydronaphthalene scaffold; Notch inhibitors; T-ALL; cancer
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