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

ACS Med Chem Lett 2019 Apr 26;10(4):639-643. Epub 2019 Feb 26.

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

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 , featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent.

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http://dx.doi.org/10.1021/acsmedchemlett.8b00608DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6466818PMC
April 2019
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