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dc.creatorRuberte, Ana Carolinaes_ES
dc.creatorPlano, Danieles_ES
dc.creatorEncío Martínez, Ignacioes_ES
dc.creatorAydillo, Carloses_ES
dc.creatorSharma, Arun K.es_ES
dc.creatorSanmartín, Carmenes_ES
dc.description.abstractTwenty-seven novel benzo[c][1,2,5]selenadiazole-5-carboxylic acid (BSCA) derivatives were designed and synthesized. Anti-proliferative activity of these structures was tested in vitro against a panel of five human cancer cell lines, including prostate (PC-3), colon (HT-29), leukemia (CCRF-CEM), lung (HTB-54) and breast (MCF-7). Four compounds (5, 6, 7 and 19) showed potent inhibitory activity with GI(50) values below 10 mu M in at least one of the cancer cell lines. The selectivity of these compounds was further examined in two non-malignant cell lines derived from breast (18465) and lung (BEAS-2B). Compound 7 exhibited promising anti-proliferative activity (GI(50) = 3.7 mu M) in MCF-7 cells, together with high selectivity index (SI> 27.1). The induction of cell death by compound 7 was independent of the apoptotic process and it did not affect cell cycle progression either. Likewise, radical scavenging properties of the new selenadiazole derivatives were confirmed by testing their ability to scavenge DPPH radicals. Four compounds (1, 2, 8 and 9) showed potent radical scavenging activity, compound 9 being the most effective. Overall, while compound 7 was identified as the most cell growth inhibitory agent and selectively toxic to cancer cells, compound 9 proved to be the most potent antioxidant among the selenadiazole derivatives synthesized. This series of compounds can serve as an excellent scaffold to achieve new and potent antioxidant compounds useful for several diseases, i.e. cancer, neurodegenerative, heart diseases and leishmaniasis, considering the high radical scavenging activity and low toxicity showed by most of the compounds.en
dc.description.sponsorshipThe authors wish to express their gratitude to the Plan de Investigacion de la Universidad de Navarra, PIUNA (Ref 2014-26), for financial support for the project. AC. Ruberte wishes to express her gratitude to the Asociacion de Amigos de la Universidad de Navarra and Caixabank for the pre-doctoral fellowship.en
dc.format.extent49 p.
dc.relation.ispartofEuropean Journal of Medicinal Chemistry, Volume 157, 5 September 2018, Pages 14-27en
dc.rights© 2018 Elsevier Masson SAS. This manuscript version is made available under the CC-BY-NC-ND 4.0.en
dc.subjectAnti-proliferative activityen
dc.subjectRadical scavengingen
dc.titleNovel selenadiazole derivatives as selective antitumor and radical scavenging agentsen
dc.typeArtículo / Artikuluaes
dc.contributor.departmentUniversidad Pública de Navarra. Departamento de Ciencias de la Saludes_ES
dc.contributor.departmentNafarroako Unibertsitate Publikoa. Osasun Zientziak Sailaeu
dc.rights.accessRightsAcceso abierto / Sarbide irekiaes
dc.type.versionVersión aceptada / Onetsi den bertsioaes

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© 2018 Elsevier Masson SAS. This manuscript version is made available under the CC-BY-NC-ND 4.0.
Except where otherwise noted, this item's license is described as © 2018 Elsevier Masson SAS. This manuscript version is made available under the CC-BY-NC-ND 4.0.