Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595974 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
A series of substituted 3-(benzylthio)-5-(1H-indol-3-yl)-4H-1,2,4-triazol-4-amines has been synthesised and tested in vitro as potential pro-apoptotic Bcl-2-inhibitory anticancer agents. Synthesis of the target compounds was readily accomplished in good yields through a cyclisation reaction between indole-3-carboxylic acid hydrazide and carbon disulfide under basic conditions, followed by S-benzylation. Active compounds, such as the nitrobenzyl analogue 6c, were found to exhibit sub-micromolar IC50 values in Bcl-2 expressing human cancer cell lines. Molecular modelling and ELISA studies further implicated anti-apoptotic Bcl-2 as a candidate molecular target underpinning anticancer activity.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Rania Hamdy, Noha Ziedan, Samia Ali, Mohamed El-Sadek, Elsaid Lashin, Andrea Brancale, Arwyn T. Jones, Andrew D. Westwell,