Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase

The growth inhibitory effect on Trypanosoma cruzi epimastigotes and the unspecific cytotoxicity over NCTC-929 fibroblasts of two series of previously synthesized 2,4-diaryl-1,2,3,4-tetrahydroquinolines (THQ), have been studied in vitro and compared with those of benznidazole (BZ). Derivatives AR39,...

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Fecha de publicación:: 2013

Institución:: Ministerio de Ciencia Tecnología e Innovación

Repositorio:: Repositorio Institucional de Minciencias

Idioma:: eng

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spelling	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidasePlantas medicinalesTrypanosoma cruziProductos químicosTrypanosoma cruziTetrahydroquinolinesCytotoxicityLipinski’s ruleOSIRIS softwareBioquímica vegetalAceites esencialesBioquímica vegetalTecnología químicaThe growth inhibitory effect on Trypanosoma cruzi epimastigotes and the unspecific cytotoxicity over NCTC-929 fibroblasts of two series of previously synthesized 2,4-diaryl-1,2,3,4-tetrahydroquinolines (THQ), have been studied in vitro and compared with those of benznidazole (BZ). Derivatives AR39, AR40, AR41, AR91 and DM15 achieved outstanding selectivity indexes (SI) on the extracellular form (SITHQ > SIBZ > 9.44) and thus, were tested in a more specific in vitro assay against amastigotes, showing less effectiveness than the reference drug (SIBZ > 320) but also accomplishing great selectivity on the intracellular stage (SITHQ > 25). These promising results, supported by the in-silico prediction of high bioavailability and less potential risk than benznidazole, reveal several tetrahydroquinolines as prototypes of potential antichagasic drugs.Departamento Administrativo de Ciencia, Tecnología e Innovación [CO] Colciencias5507-543-31904Programa: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombianano2019-04-01T04:04:47Z2019-04-01T04:04:47Z2013-07info:eu-repo/date/embargoEnd/2024-01-31Artículo científicoinfo:eu-repo/semantics/articlehttp://purl.org/coar/version/c_970fb48d4fbd8a85http://purl.org/coar/resource_type/c_2df8fbb1pdf6 páginasapplication/pdf0960-894Xhttp://repositorio.colciencias.gov.co/handle/11146/34187Contiene 50 referencias bibliográficas. Véase documento adjunto10.1016/j.bmcl.2013.06.079Bioorganic & Medicinal Chemistry Letters 23 (2013) 4851-4856engPrograma: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombiana. La publicación completa está disponible en : <a href="http://repositorio.colciencias.gov.co/handle/11146/34163" target="blank">http://repositorio.colciencias.gov.co/handle/11146/34163</a>Colombiahttp://purl.org/coar/access_right/c_f1cfFonseca Berzal, CristinaMerchan Arenas, Diego RolandoRomero Bohórquez, Arnold R.Escario, José A.Kouznetsov, Vladimir V.Gómez Barrio, Aliciaoai:repositorio.minciencias.gov.co:20.500.14143/341872023-11-29T17:45:56Z
dc.title.none.fl_str_mv	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase
title	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase
spellingShingle	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase Plantas medicinales Trypanosoma cruzi Productos químicos Trypanosoma cruzi Tetrahydroquinolines Cytotoxicity Lipinski’s rule OSIRIS software Bioquímica vegetal Aceites esenciales Bioquímica vegetal Tecnología química
title_short	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase
title_full	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase
title_fullStr	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase
title_full_unstemmed	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase
title_sort	Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase
dc.subject.none.fl_str_mv	Plantas medicinales Trypanosoma cruzi Productos químicos Trypanosoma cruzi Tetrahydroquinolines Cytotoxicity Lipinski’s rule OSIRIS software Bioquímica vegetal Aceites esenciales Bioquímica vegetal Tecnología química
topic	Plantas medicinales Trypanosoma cruzi Productos químicos Trypanosoma cruzi Tetrahydroquinolines Cytotoxicity Lipinski’s rule OSIRIS software Bioquímica vegetal Aceites esenciales Bioquímica vegetal Tecnología química
description	The growth inhibitory effect on Trypanosoma cruzi epimastigotes and the unspecific cytotoxicity over NCTC-929 fibroblasts of two series of previously synthesized 2,4-diaryl-1,2,3,4-tetrahydroquinolines (THQ), have been studied in vitro and compared with those of benznidazole (BZ). Derivatives AR39, AR40, AR41, AR91 and DM15 achieved outstanding selectivity indexes (SI) on the extracellular form (SITHQ > SIBZ > 9.44) and thus, were tested in a more specific in vitro assay against amastigotes, showing less effectiveness than the reference drug (SIBZ > 320) but also accomplishing great selectivity on the intracellular stage (SITHQ > 25). These promising results, supported by the in-silico prediction of high bioavailability and less potential risk than benznidazole, reveal several tetrahydroquinolines as prototypes of potential antichagasic drugs.
publishDate	2013
dc.date.none.fl_str_mv	2013-07 2019-04-01T04:04:47Z 2019-04-01T04:04:47Z info:eu-repo/date/embargoEnd/2024-01-31
dc.type.none.fl_str_mv	Artículo científico info:eu-repo/semantics/article
dc.type.coarversion.fl_str_mv	http://purl.org/coar/version/c_970fb48d4fbd8a85
dc.type.coar.fl_str_mv	http://purl.org/coar/resource_type/c_2df8fbb1
dc.identifier.none.fl_str_mv	0960-894X http://repositorio.colciencias.gov.co/handle/11146/34187 Contiene 50 referencias bibliográficas. Véase documento adjunto 10.1016/j.bmcl.2013.06.079
identifier_str_mv	0960-894X Contiene 50 referencias bibliográficas. Véase documento adjunto 10.1016/j.bmcl.2013.06.079
url	http://repositorio.colciencias.gov.co/handle/11146/34187
dc.language.none.fl_str_mv	eng
language	eng
dc.relation.none.fl_str_mv	Programa: Bioprospección y desarrollo de ingredientes naturales para las industrias cosmética, farmacéutica y de productos de aseo con base en la biodiversidad colombiana. La publicación completa está disponible en : <a href="http://repositorio.colciencias.gov.co/handle/11146/34163" target="blank">http://repositorio.colciencias.gov.co/handle/11146/34163</a>
dc.rights.coar.fl_str_mv	http://purl.org/coar/access_right/c_f1cf
rights_invalid_str_mv	http://purl.org/coar/access_right/c_f1cf
dc.format.none.fl_str_mv	pdf 6 páginas application/pdf
dc.coverage.none.fl_str_mv	Colombia
dc.source.none.fl_str_mv	Bioorganic & Medicinal Chemistry Letters 23 (2013) 4851-4856
institution	Ministerio de Ciencia Tecnología e Innovación
repository.name.fl_str_mv
repository.mail.fl_str_mv
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Selective activity of 2,4-diaryl-1,2,3,4-tetrahydroquinolines on Trypanosoma cruzi epimastigotes and amastigotes expressing β-galactosidase

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