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

Author:
Quaglio, Deborah; Zhdanovskaya, Nadezda; Tobajas, Gloria; Cuartas, Viviana; Balducci, Silvia; [et al.]
URI:
https://hdl.handle.net/20.500.12412/7040
ISSN:
1948-5875
DOI:
10.1021/acsmedchemlett.8b00608
Date:
2019-02-26
Keyword(s):

Chalcone

tetrahydronaphthalene scaffold

Notch inhibitors

T-ALL

cancer

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.

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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Attribution-NonCommercial-NoDerivatives 4.0 Internacional
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivatives 4.0 Internacional