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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:20

Article

Romagnoli, Romeo¹  Baraldi, Pier Giovanni¹  Cruz-Lopez, Olga¹  Cara, Carlota Lopez¹  Carrion, Maria Dora¹  Balzarini, Jan²  Hamel, Ernest³  Basso, Giuseppe⁴  Bortolozzi, Roberta⁴  Viola, Giampietro⁴ 

[1] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy

[2] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, B-3000 Louvain, Belgium

[3] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA

[4] Univ Padua, Dipartimento Pediat, Lab Oncoematol, I-35131 Padua, Italy

关键词: Antiproliferative activity;    Apoptosis;    Antitumor agents;    Hybrid compounds;   

DOI  :  10.1016/j.bmcl.2010.03.075

来源: Elsevier

【 摘 要 】

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. (C) 2010 Elsevier Ltd. All rights reserved.

【 授权许可】

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