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


Journal

ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073

Informations de publication

Date de publication:
11 Apr 2019
Historique:
received: 30 11 2018
accepted: 26 02 2019
entrez: 19 4 2019
pubmed: 19 4 2019
medline: 19 4 2019
Statut: epublish

Résumé

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

Identifiants

pubmed: 30996810
doi: 10.1021/acsmedchemlett.8b00608
pmc: PMC6466818
doi:

Types de publication

Journal Article

Langues

eng

Pagination

639-643

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Deborah Quaglio (D)

Department of Chemistry and Technology of Drugs, "Department of Excellence 2018-2022", Sapienza Università di Roma, P.le Aldo Moro 5, 00185 Rome, Italy.

Nadezda Zhdanovskaya (N)

Department of Molecular Medicine, Sapienza University, 00161 Rome, Italy.

Gloria Tobajas (G)

Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.

Viviana Cuartas (V)

Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.

Silvia Balducci (S)

Department of Chemistry and Technology of Drugs, "Department of Excellence 2018-2022", Sapienza Università di Roma, P.le Aldo Moro 5, 00185 Rome, Italy.

Michael S Christodoulou (MS)

DISFARM, Sezione di Chimica Generale e Organica "A. Marchesini", Università degli Studi di Milano, Via Venezian 21, 20133 Milano, Italy.

Giancarlo Fabrizi (G)

Department of Chemistry and Technology of Drugs, "Department of Excellence 2018-2022", Sapienza Università di Roma, P.le Aldo Moro 5, 00185 Rome, Italy.

Marta Gargantilla (M)

Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.

Eva-María Priego (EM)

Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.

Álvaro Carmona Pestaña (Á)

Department of Molecular Medicine, Sapienza University, 00161 Rome, Italy.

Daniele Passarella (D)

Dipartimento di Chimica, Università degli Studi di Milano, Via Golgi, 19, 20133 Milano, Italy.

Isabella Screpanti (I)

Department of Molecular Medicine, Sapienza University, 00161 Rome, Italy.

Bruno Botta (B)

Department of Chemistry and Technology of Drugs, "Department of Excellence 2018-2022", Sapienza Università di Roma, P.le Aldo Moro 5, 00185 Rome, Italy.

Rocco Palermo (R)

Department of Molecular Medicine, Sapienza University, 00161 Rome, Italy.

Mattia Mori (M)

Department of Biotechnology, Chemistry and Pharmacy, "Department of Excellence 2018-2022", University of Siena, via Aldo Moro 2, 53100 Siena, Italy.

Francesca Ghirga (F)

Center for Life Nano Science@Sapienza, Istituto Italiano di Tecnologia, Viale Regina Elena 291, 00161 Rome, Italy.

María-Jesús Pérez-Pérez (MJ)

Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.

Classifications MeSH