Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives

Ehrsam, Daniel and Porta, Fabiola and Mori, Matteo and Meyer zu Schwabedissen, Henriette E. and Dalla Via, Lisa and Garcia-Argaez, Aìda Nelly and Basile, Livia and Meneghetti, Fiorella and Villa, Stefania and Gelain, Arianna. (2019) Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives. Anticancer Research, 39 (7). pp. 3453-3461.

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Official URL: https://edoc.unibas.ch/71563/

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To develop several new derivatives aimed to complete the studies concerning the antiproliferative profile of the oxadiazole derivative MD77.; The substitution pattern around the phenyl rings of this compound was analyzed through the synthesis of positional isomers and of analogues bearing different substituents at the para positions (; 2-12; ).; The results of the antiproliferative activity of these derivatives versus HCT-116 and HeLa cancer cell lines shed light on the effects of the presence, nature and position of such substituents. Notably, derivative; 4; , a regioisomer of; 1; in which the substituents at the para positions of the phenyl rings were inverted, showed the best antiproliferative profile, exhibiting a significant activity also against MCF7 and MDA-MB 468 cancer cell lines.; Preliminary results showed the ability of compound; 4; to reduce the viability of cancer cells by counteracting human recombinant topoisomerase II α relaxation activity.
Faculties and Departments:05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Biopharmacy (Meyer zu Schwabedissen)
UniBasel Contributors:Meyer zu Schwabedissen, Henriette and Ehrsam, Daniel and Porta, Fabiola
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Stanford University Highwire Press
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:17 Aug 2020 15:21
Deposited On:17 Aug 2020 15:21

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