Hamdy, Rania, Ziedan, Noha, Ali, Samia, El-Sadek, Mohamed, Lashin, Elsaid, Brancale, Andrea  ORCID: https://orcid.org/0000-0002-9728-3419, Jones, Arwyn Tomos ORCID: https://orcid.org/0000-0003-2781-8905 and Westwell, Andrew D. ORCID: https://orcid.org/0000-0002-5166-9236
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
|
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: | 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: | 05 Jan 2024 05:53 |
| URI: | https://orca.cardiff.ac.uk/id/eprint/45942 |
Citation Data
Cited 24 times in Scopus. View in Scopus. Powered By Scopus® Data
Actions (repository staff only)
 |
Edit Item |
Dimensions
Dimensions