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

AuthorsQuaglio, D.; Zhdanovskaya, N.; Tobajas, Gloria; Cuartas, V.; Balducci, S.; Christodoulou, M. S.; Fabrizi, G.; Gargantilla, Marta; Priego, Eva María ; Carmona Pestania, Á.; Passarella, D.; Screpanti, I.; Botta, B.; Palermo, R.; Mori, M.; Ghirga, F.; Peréz-Pérez, María-Jesús
Notch inhibitors, T-ALL
Tetrahydronaphthalene scaffold
Issue Date2019
PublisherAmerican Chemical Society
CitationACS Medicinal Chemistry Letters 10: 639-643 (2019)
AbstractBased 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.
Publisher version (URL)http://dx.doi.org/10.1021/acsmedchemlett.8b00608
Identifiersdoi: 10.1021/acsmedchemlett.8b00608
issn: 1948-5875
e-issn: 1948-5875
Appears in Collections:(IQM) Artículos
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