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Symmetrical alpha-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation.

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.

SUBMITTER: Romagnoli R

PROVIDER: S-EPMC2864628 | biostudies-literature | 2010 May

REPOSITORIES: biostudies-literature

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Symmetrical alpha-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation.

Romagnoli Romeo R Baraldi Pier Giovanni PG Cruz-Lopez Olga O Lopez Cara Carlota C Carrion Maria Dora MD Balzarini Jan J Hamel Ernest E Basso Giuseppe G Bortolozzi Roberta R Viola Giampietro G

Bioorganic & medicinal chemistry letters 20100325 9

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 concentra ...[more]

PMID: 20378350

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