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 / Quaglio, D., Zhdanovskaya, N., Tobajas, G., Cuartas, V., Balducci, S., Christodoulou, M.S., Fabrizi, G., Gargantilla, M., Priego, E., CARMONA PESTAñA, A., Passarella, D., Screpanti, I., Botta, B., Palermo, R., Mori, M., Ghirga, F., Pérez-Pérez, M.. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - 10:4(2019), pp. 639-643. [10.1021/acsmedchemlett.8b00608]
Chalcones and chalcone-mimetic derivatives as Notch inhibitors in a model of T-cell Acute Lymphoblastic Leukemia
Quaglio, DeborahCo-primo
;Zhdanovskaya, NadezdaCo-primo
;BALDUCCI, Silvia;Fabrizi, Giancarlo;CARMONA PESTAñA, ALVARO;PASSARELLA, DANIELE;Screpanti, Isabella;Botta, Bruno;Palermo, Rocco
;Mori, Mattia
;Ghirga, Francesca
;
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.| File | Dimensione | Formato | |
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