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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

Hamdy, Rania, Ziedan, Noha, Ali, Samia, El-Sadek, Mohamed, Lashin, Elsaid, Brancale, Andrea, Jones, Arwyn Tomos and Westwell, Andrew D. 2013. Synthesis and evaluation of 3-(benzylthio)-5-(1H-indol-3-yl)-1,2,4-triazol-4-amines as Bcl-2 inhibitory anticancer agents. Biorganic and Medicinal Chemistry Letters 23 (8) , pp. 2391-2394. 10.1016/j.bmcl.2013.02.029

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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.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
R Medicine > RS Pharmacy and materia medica
Uncontrolled Keywords: Anti-apoptotic Bcl-2; Anticancer; Indoles; Triazole-amines
Publisher: Elsevier
ISSN: 0960-894X
Last Modified: 12 Sep 2019 21:25
URI: http://orca.cf.ac.uk/id/eprint/45942

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