Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity

Pérez-Silanes, S. (Silvia)|||/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45; Torres, E. (Enrique)|||/items/63f6c247-849f-4192-9a16-b86398ba3fc5; Arbillaga, L. (Leire)|||/items/5d121cf6-ae3a-49f1-853d-2bcd4588ff39; Varela, J. (Javier)|||/items/f43d2ac4-3cc7-492e-87ce-4fbbd3502a24; Cerecetto, H. (Hugo)|||/items/1523fcc1-ed1c-48ee-af83-bb942d02b04c; Gonzalez, M. (Mercedes)|||/items/45aefdd5-3d3d-4bfa-bb92-3aecbf81f554; Azqueta, A. (Amaya)|||/items/f04b3c23-3ff4-41c8-b5e1-4d372fbc4893; Moreno-de-Viguri, E. (Elsa)|||/items/08473f69-a6ab-4896-8cf9-41e6daf12bfa

Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity

Abstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cytot...

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Detalles Bibliográficos
Autores:	Pérez-Silanes, S. (Silvia)\|\|\|/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45, Torres, E. (Enrique)\|\|\|/items/63f6c247-849f-4192-9a16-b86398ba3fc5, Arbillaga, L. (Leire)\|\|\|/items/5d121cf6-ae3a-49f1-853d-2bcd4588ff39, Varela, J. (Javier)\|\|\|/items/f43d2ac4-3cc7-492e-87ce-4fbbd3502a24, Cerecetto, H. (Hugo)\|\|\|/items/1523fcc1-ed1c-48ee-af83-bb942d02b04c, Gonzalez, M. (Mercedes)\|\|\|/items/45aefdd5-3d3d-4bfa-bb92-3aecbf81f554, Azqueta, A. (Amaya)\|\|\|/items/f04b3c23-3ff4-41c8-b5e1-4d372fbc4893, Moreno-de-Viguri, E. (Elsa)\|\|\|/items/08473f69-a6ab-4896-8cf9-41e6daf12bfa
Tipo de recurso:	artículo
Fecha de publicación:	2016
País:	España
Institución:	Universidad de Navarra
Repositorio:	Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:	inglés
OAI Identifier:	oai:dadun.unav.edu:10171/40413
Acceso en línea:	https://hdl.handle.net/10171/40413
Access Level:	acceso abierto
Palabra clave:	Chagas disease Trypanosoma cruzi Quinoxaline N-oxide Cytotoxicity Genotoxicity Materias Investigacion::Farmacia::Química farmacéutica Materias Investigacion::Farmacia::Farmacia y farmacología

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spelling	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activityPérez-Silanes, S. (Silvia)\|\|\|/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45Torres, E. (Enrique)\|\|\|/items/63f6c247-849f-4192-9a16-b86398ba3fc5Arbillaga, L. (Leire)\|\|\|/items/5d121cf6-ae3a-49f1-853d-2bcd4588ff39Varela, J. (Javier)\|\|\|/items/f43d2ac4-3cc7-492e-87ce-4fbbd3502a24Cerecetto, H. (Hugo)\|\|\|/items/1523fcc1-ed1c-48ee-af83-bb942d02b04cGonzalez, M. (Mercedes)\|\|\|/items/45aefdd5-3d3d-4bfa-bb92-3aecbf81f554Azqueta, A. (Amaya)\|\|\|/items/f04b3c23-3ff4-41c8-b5e1-4d372fbc4893Moreno-de-Viguri, E. (Elsa)\|\|\|/items/08473f69-a6ab-4896-8cf9-41e6daf12bfaChagas diseaseTrypanosoma cruziQuinoxaline N-oxideCytotoxicityGenotoxicityMaterias Investigacion::Farmacia::Química farmacéuticaMaterias Investigacion::Farmacia::Farmacia y farmacologíaAbstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening.ElsevierDadun. Depósito Académico Digital Universidad de Navarra20162016-04-2520162016-01-0120162016-01-01journal articlehttp://purl.org/coar/resource_type/c_6501info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/10171/40413reponame:Dadun. Depósito Académico Digital de la Universidad de Navarrainstname:Universidad de NavarraInglésengopen accesshttp://purl.org/coar/access_right/c_abf2info:eu-repo/semantics/openAccessoai:dadun.unav.edu:10171/404132026-06-21T12:47:57Z
dc.title.none.fl_str_mv	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
title	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
spellingShingle	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity Pérez-Silanes, S. (Silvia)\|\|\|/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45 Chagas disease Trypanosoma cruzi Quinoxaline N-oxide Cytotoxicity Genotoxicity Materias Investigacion::Farmacia::Química farmacéutica Materias Investigacion::Farmacia::Farmacia y farmacología
title_short	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
title_full	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
title_fullStr	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
title_full_unstemmed	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
title_sort	Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity
dc.creator.none.fl_str_mv	Pérez-Silanes, S. (Silvia)\|\|\|/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45 Torres, E. (Enrique)\|\|\|/items/63f6c247-849f-4192-9a16-b86398ba3fc5 Arbillaga, L. (Leire)\|\|\|/items/5d121cf6-ae3a-49f1-853d-2bcd4588ff39 Varela, J. (Javier)\|\|\|/items/f43d2ac4-3cc7-492e-87ce-4fbbd3502a24 Cerecetto, H. (Hugo)\|\|\|/items/1523fcc1-ed1c-48ee-af83-bb942d02b04c Gonzalez, M. (Mercedes)\|\|\|/items/45aefdd5-3d3d-4bfa-bb92-3aecbf81f554 Azqueta, A. (Amaya)\|\|\|/items/f04b3c23-3ff4-41c8-b5e1-4d372fbc4893 Moreno-de-Viguri, E. (Elsa)\|\|\|/items/08473f69-a6ab-4896-8cf9-41e6daf12bfa
author	Pérez-Silanes, S. (Silvia)\|\|\|/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45
author_facet	Pérez-Silanes, S. (Silvia)\|\|\|/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45 Torres, E. (Enrique)\|\|\|/items/63f6c247-849f-4192-9a16-b86398ba3fc5 Arbillaga, L. (Leire)\|\|\|/items/5d121cf6-ae3a-49f1-853d-2bcd4588ff39 Varela, J. (Javier)\|\|\|/items/f43d2ac4-3cc7-492e-87ce-4fbbd3502a24 Cerecetto, H. (Hugo)\|\|\|/items/1523fcc1-ed1c-48ee-af83-bb942d02b04c Gonzalez, M. (Mercedes)\|\|\|/items/45aefdd5-3d3d-4bfa-bb92-3aecbf81f554 Azqueta, A. (Amaya)\|\|\|/items/f04b3c23-3ff4-41c8-b5e1-4d372fbc4893 Moreno-de-Viguri, E. (Elsa)\|\|\|/items/08473f69-a6ab-4896-8cf9-41e6daf12bfa
author_role	author
author2	Torres, E. (Enrique)\|\|\|/items/63f6c247-849f-4192-9a16-b86398ba3fc5 Arbillaga, L. (Leire)\|\|\|/items/5d121cf6-ae3a-49f1-853d-2bcd4588ff39 Varela, J. (Javier)\|\|\|/items/f43d2ac4-3cc7-492e-87ce-4fbbd3502a24 Cerecetto, H. (Hugo)\|\|\|/items/1523fcc1-ed1c-48ee-af83-bb942d02b04c Gonzalez, M. (Mercedes)\|\|\|/items/45aefdd5-3d3d-4bfa-bb92-3aecbf81f554 Azqueta, A. (Amaya)\|\|\|/items/f04b3c23-3ff4-41c8-b5e1-4d372fbc4893 Moreno-de-Viguri, E. (Elsa)\|\|\|/items/08473f69-a6ab-4896-8cf9-41e6daf12bfa
author2_role	author author author author author author author
dc.contributor.none.fl_str_mv	Dadun. Depósito Académico Digital Universidad de Navarra
dc.subject.none.fl_str_mv	Chagas disease Trypanosoma cruzi Quinoxaline N-oxide Cytotoxicity Genotoxicity Materias Investigacion::Farmacia::Química farmacéutica Materias Investigacion::Farmacia::Farmacia y farmacología
topic	Chagas disease Trypanosoma cruzi Quinoxaline N-oxide Cytotoxicity Genotoxicity Materias Investigacion::Farmacia::Química farmacéutica Materias Investigacion::Farmacia::Farmacia y farmacología
description	Abstract: We report the synthesis and in vitro activity against T. cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 M. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening.
publishDate	2016
dc.date.none.fl_str_mv	2016 2016-04-25 2016 2016-01-01 2016 2016-01-01
dc.type.none.fl_str_mv	journal article http://purl.org/coar/resource_type/c_6501
dc.type.openaire.fl_str_mv	info:eu-repo/semantics/article
format	article
dc.identifier.none.fl_str_mv	https://hdl.handle.net/10171/40413
url	https://hdl.handle.net/10171/40413
dc.language.none.fl_str_mv	Inglés eng
language_invalid_str_mv	Inglés
language	eng
dc.rights.none.fl_str_mv	open access http://purl.org/coar/access_right/c_abf2
dc.rights.openaire.fl_str_mv	info:eu-repo/semantics/openAccess
rights_invalid_str_mv	open access http://purl.org/coar/access_right/c_abf2
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:Dadun. Depósito Académico Digital de la Universidad de Navarra instname:Universidad de Navarra
instname_str	Universidad de Navarra
reponame_str	Dadun. Depósito Académico Digital de la Universidad de Navarra
collection	Dadun. Depósito Académico Digital de la Universidad de Navarra
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Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity

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