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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Romagnoli R,Baraldi PG,Cruz-Lopez O,Lopez Cara C,Carrion MD,Balzarini J,Hamel E,Basso G,Bortolozzi R,Viola G

doi

10.1016/j.bmcl.2010.03.075

subject

Has Abstract

pub_date

2010-05-01 00:00:00

pages

2733-9

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00406-3

journal_volume

20

pub_type

杂志文章

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