Title: Symmetrical alpha-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation
Authors: Romagnoli, Romeo ×
Baraldi, Pier Giovanni
Cruz-Lopez, Olga
Lopez Cara, Carlota
Carrion, Maria Dora
Balzarini, Jan
Hamel, Ernest
Basso, Giuseppe
Bortolozzi, Roberta
Viola, Giampietro #
Issue Date: May-2010
Publisher: Pergamon Press
Series Title: Bioorganic & Medicinal Chemistry Letters vol:20 issue:9 pages:2733-9
Abstract: In a continuing study of hybrid compounds containing the alpha-bromoacryloyl moiety as potential anticancer drugs, we synthesized a novel series of hybrids 4a-h, in which this moiety was linked to a 1,5-diaryl-1,4-pentadien-3-one system. Many of the conjugates prepared (4b, 4c, 4e and 4g) demonstrated pronounced, submicromolar antiproliferative activity against four cancer cell lines. Moreover, compound 4b induced apoptosis through the mitochondrial pathway and activated caspase-3 in a concentration-dependent manner.
ISSN: 0960-894X
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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