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

Alexander Ciupa, Natalie J Griffiths, Stephanie K Light, Pauline J Wood, Lorenzo Caggiano

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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).
Original languageEnglish
Pages (from-to)1011-1015
Number of pages5
JournalMedChemComm
Volume2
Issue number10
Early online date4 Sep 2011
DOIs
Publication statusPublished - 1 Oct 2011

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