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Title: Synthesis and antiproliferative activity of novel heterocyclic Glycyrrhetinic acid derivatives
Author: Alho, Daniela P.S.
Salvador, Jorge A.R.
Cascante i Serratosa, Marta
Marín Martínez, Silvia
Keywords: Apoptosi
Issue Date: 20-Feb-2019
Publisher: MDPI
Abstract: A new series of glycyrrhetinic acid derivatives has been synthesized via the introduction of different heterocyclic rings conjugated with an α,β-unsaturated ketone in its ring A. These new compounds were screened for their antiproliferative activity in a panel of nine human cancer cell lines. Compound 10 was the most active derivative, with an IC50 of 1.1 µM on Jurkat cells, which is 96-fold more potent than that of glycyrrhetinic acid, and was 4-fold more selective toward that cancer cell line. Further biological studies performed in Jurkat cells showed that compound 10 is a potent inducer of apoptosis that activates both the intrinsic and extrinsic pathways.
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It is part of: Molecules, 2019, vol. 24, num. 4, p. 766
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ISSN: 1420-3049
Appears in Collections:Articles publicats en revistes (Bioquímica i Biomedicina Molecular)

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