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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

SJR Quartile

JCR Impact

3.975

SJR Impact

1.158

Publication date

01/04/2019

ISI

000464767700043

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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