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Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
ID 4510266
Author(s) Ehrsam, Daniel; Porta, Fabiola; Mori, Matteo; Meyer zu Schwabedissen, Henriette E.; Dalla Via, Lisa; Garcia-Argaez, Ažda Nelly; Basile, Livia; Meneghetti, Fiorella; Villa, Stefania; Gelain, Arianna
Author(s) at UniBasel Meyer zu Schwabedissen, Henriette
Ehrsam, Daniel
Porta, Fabiola
Year 2019
Title Unravelling the Antiproliferative Activity of 1,2,5-oxadiazole Derivatives
Journal Anticancer Research
Volume 39
Number 7
Pages / Article-Number 3453-3461
Keywords Furazane; HCT-116; HeLa; MCF-7; MDA-MB 468; cytotoxicity; topoisomerase II
Mesh terms Antineoplastic Agents, pharmacology; Cell Line, Tumor; Cell Proliferation, drug effects; Humans; Oxadiazoles, pharmacology
Abstract 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.
Publisher Stanford University Highwire Press
ISSN/ISBN 0250-7005 ; 1791-7530
Full Text on edoc No
Digital Object Identifier DOI 10.21873/anticanres.13491
PubMed ID

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