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


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.

SUBMITTER: Quaglio D 

PROVIDER: S-EPMC6466818 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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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 <b>18</b>, featuring a tetrahydronaphthalene-based scaffold, as a new promising Notch-blocking agent. ...[more]