Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia
| Autor: | Giancarlo Fabrizi, Daniele Passarella, Viviana Cuartas, Gloria Tobajas, Isabella Screpanti, Francesca Ghirga, Michael S. Christodoulou, Eva-María Priego, Marta Gargantilla, Bruno Botta, Mattia Mori, Deborah Quaglio, Silvia Balducci, Álvaro Carmona Pestaña, Rocco Palermo, María-Jesús Pérez-Pérez, Nadezda Zhdanovskaya |
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| Přispěvatelé: | European Commission, Sapienza Università di Roma, Ministerio de Economía y Competitividad (España) |
| Rok vydání: | 2019 |
| Předmět: |
Chalcone
T cell Lymphoblastic Leukemia Notch inhibitors 01 natural sciences Biochemistry chemistry.chemical_compound Drug Discovery Notch inhibitors T-ALL medicine cancer Cancer tetrahydronaphthalene scaffold 010405 organic chemistry Chemistry T-ALL Organic Chemistry 0104 chemical sciences 010404 medicinal & biomolecular chemistry medicine.anatomical_structure Cell culture Chemical diversity Cancer research Antiproliferative effect Tetrahydronaphthalene scaffold |
| Zdroj: | Digital.CSIC. Repositorio Institucional del CSIC instname |
| Popis: | 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. The authors acknowledge networking contribution by the COST Action CM1407 “Challenging organic syntheses inspired by nature - from natural products chemistry to drug discovery”. V.C. thanks the Universidad del Valle (CIAM- 2017) and the Science, Technology and Innovation Fund- General Royalties System (FCTeI-SGR) under contract BPIN 2013000100007 for a predoctoral fellowship. This work has been supported by Italian Ministry of Education, University and Research - Dipartimenti di Eccellenza - L. 232/2016. This work has been partially supported by a grant from MINECO/ FEDER SAF2015-64629-C2-1-R (to M-J.P.-P and E-M.P), MIUR PNR 2015−2020 (ARS01_00432) (to I.S.), and Sapienza University 2016 Project number RG116154E2- C7A6FB (to I.S.). |
| Databáze: | OpenAIRE |
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