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Issue 10, 2011
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Design, synthesis and antiproliferative activity of urocanic-chalcone hybrid derivatives

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Abstract

Inspired by biologically active natural products, a hybrid analogue that combines the N-Me urocanic side chain of the sarcodictyin family of compounds with the chalcone motif has been proposed, synthesised and examined for antiproliferative activity in three cancer cell lines and one normal primary cell line. The analogues are all synthesised in one or two steps from commercially available materials and, of the compounds examined, the proposed hybrid analogue displays the most active and selective inhibition of cell proliferation in human colon cancer cell line HT29 (IC50 2.9 μM) and highly metastatic human breast carcinoma MDA-MB-231 (IC50 4.8 μM).

Graphical abstract: Design, synthesis and antiproliferative activity of urocanic-chalcone hybrid derivatives

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Publication details

The article was received on 16 Jun 2011, accepted on 30 Jul 2011 and first published on 05 Sep 2011


Article type: Concise Article
DOI: 10.1039/C1MD00155H
Citation: Med. Chem. Commun., 2011,2, 1011-1015
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    Design, synthesis and antiproliferative activity of urocanic-chalcone hybrid derivatives

    A. Ciupa, N. J. Griffiths, S. K. Light, P. J. Wood and L. Caggiano, Med. Chem. Commun., 2011, 2, 1011
    DOI: 10.1039/C1MD00155H

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