Design, synthesis and pro-apoptotic antitumour properties of indole-based 3,5-disubstituted oxadiazoles

Ziedan, Noha I., Stefanelli, Fabio, Fogli, Stefano and Westwell, Andrew D. ORCID: https://orcid.org/0000-0002-5166-9236 2010. Design, synthesis and pro-apoptotic antitumour properties of indole-based 3,5-disubstituted oxadiazoles. European Journal of Medicinal Chemistry 45 (10) , pp. 4523-4530. 10.1016/j.ejmech.2010.07.012

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Abstract

A series of new indole-based 3,5-disubstituted 1,2,4-oxadiazoles has been designed and synthesised as potential pro-apoptotic antitumour agents, via the base-catalysed condensation reaction between substituted amidoximes and indole esters. Evaluation of antiproliferative activity against the human cancer cell lines COLO 320 (colorectal) and MIA PACA-2 (pancreatic) revealed IC(50) values in the low micromolar range. Selected compounds were able to trigger apoptosis in sensitive cell lines, for example via activation of caspase-3/7, demonstrating that indole-based oxadiazoles possess in vitro antitumour and pro-apoptotic activity.

Item Type:	Article
Date Type:	Publication
Status:	Published
Schools:	Pharmacy
Subjects:	R Medicine > RS Pharmacy and materia medica
Publisher:	Elsevier
ISSN:	0223-5234
Last Modified:	19 Oct 2022 09:02
URI:	https://orca.cardiff.ac.uk/id/eprint/19768

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