Novel selenadiazole derivatives as selective antitumor and radical scavenging agents

Twenty-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...

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Autores: Ruberte, Ana Carolina, Plano, Daniel, Encío Martínez, Ignacio, Aydillo, Carlos, Sharma, Arun K., Sanmartín, Carmen
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2018
País:España
Institución:Universidad Pública de Navarra
Repositorio:Academica-e. Repositorio Institucional de la Universidad Pública de Navarra
OAI Identifier:oai:academica-e.unavarra.es:2454/33733
Acceso en línea:https://hdl.handle.net/2454/33733
Access Level:acceso abierto
Palabra clave:Anti-proliferative activity
Radical scavenging
Selenadiazole
Selenium
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spelling Novel selenadiazole derivatives as selective antitumor and radical scavenging agentsRuberte, Ana CarolinaPlano, DanielEncío Martínez, IgnacioAydillo, CarlosSharma, Arun K.Sanmartín, CarmenAnti-proliferative activityRadical scavengingSelenadiazoleSeleniumTwenty-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.The 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.ElsevierCiencias de la SaludOsasun Zientziak2018info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfhttps://hdl.handle.net/2454/33733reponame:Academica-e. Repositorio Institucional de la Universidad Pública de Navarrainstname:Universidad Pública de NavarraInglés© 2018 Elsevier Masson SAS. This manuscript version is made available under the CC-BY-NC-ND 4.0.https://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessoai:academica-e.unavarra.es:2454/337332026-06-17T12:41:47Z
dc.title.none.fl_str_mv Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
title Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
spellingShingle Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
Ruberte, Ana Carolina
Anti-proliferative activity
Radical scavenging
Selenadiazole
Selenium
title_short Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
title_full Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
title_fullStr Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
title_full_unstemmed Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
title_sort Novel selenadiazole derivatives as selective antitumor and radical scavenging agents
dc.creator.none.fl_str_mv Ruberte, Ana Carolina
Plano, Daniel
Encío Martínez, Ignacio
Aydillo, Carlos
Sharma, Arun K.
Sanmartín, Carmen
author Ruberte, Ana Carolina
author_facet Ruberte, Ana Carolina
Plano, Daniel
Encío Martínez, Ignacio
Aydillo, Carlos
Sharma, Arun K.
Sanmartín, Carmen
author_role author
author2 Plano, Daniel
Encío Martínez, Ignacio
Aydillo, Carlos
Sharma, Arun K.
Sanmartín, Carmen
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Ciencias de la Salud
Osasun Zientziak
dc.subject.none.fl_str_mv Anti-proliferative activity
Radical scavenging
Selenadiazole
Selenium
topic Anti-proliferative activity
Radical scavenging
Selenadiazole
Selenium
description Twenty-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.
publishDate 2018
dc.date.none.fl_str_mv 2018
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/2454/33733
url https://hdl.handle.net/2454/33733
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.rights.none.fl_str_mv © 2018 Elsevier Masson SAS. This manuscript version is made available under the CC-BY-NC-ND 4.0.
https://creativecommons.org/licenses/by-nc-nd/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv © 2018 Elsevier Masson SAS. This manuscript version is made available under the CC-BY-NC-ND 4.0.
https://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:Academica-e. Repositorio Institucional de la Universidad Pública de Navarra
instname:Universidad Pública de Navarra
instname_str Universidad Pública de Navarra
reponame_str Academica-e. Repositorio Institucional de la Universidad Pública de Navarra
collection Academica-e. Repositorio Institucional de la Universidad Pública de Navarra
repository.name.fl_str_mv
repository.mail.fl_str_mv
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