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.
Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia / D. Quaglio, N. Zhdanovskaya, G. Tobajas, V. Cuartas, S. Balducci, M.S. Christodoulou, G. Fabrizi, M. Gargantilla, E.-. Priego, A. Carmona Pestania, D. Passarella, I. Screpanti, B. Botta, R. Palermo, M. Mori, F. Ghirga, M.-. Perez-Perez. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 10:4(2019 Apr 11), pp. 639-643. [10.1021/acsmedchemlett.8b00608]
Chalcones and Chalcone-mimetic Derivatives as Notch Inhibitors in a Model of T-cell Acute Lymphoblastic Leukemia
M.S. Christodoulou;D. Passarella;
2019
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.
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