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Synthesis and evaluation of 3-(benzylthio)-5-(1H-indol-3-yl)-1,2,4-triazol-4-amines as Bcl-2 inhibitory anticancer agents
Faculty
Pharmacy
Year:
2013
Type of Publication:
Article
Pages:
2391-2394
Authors:
Brancale, Andrea, Jones, Arwyn T, Westwell, Andrew D, El-Sadek, Mohamed, Hamdy, Rania, Ziedan, Noha, Ali, Samia, Lashin, Elsaid
DOI:
10.1016/j.bmcl.2013.02.029
Journal:
BIOORGANIC \& MEDICINAL CHEMISTRY LETTERS PERGAMON-ELSEVIER SCIENCE LTD
Volume:
23
Research Area:
Pharmacology \& Pharmacy; Chemistry
ISSN
ISI:000316934000024
Keywords :
Anti-apoptotic Bcl-2, Anticancer, Indoles, Triazole-amines
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. (C) 2013 Elsevier Ltd. All rights reserved.
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