2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells

Autores
Despaigne, Angel A. R.; Parrilha, Gabrieli L.; Izidoro, Jans B.; da Costa, Pryscila R.; dos Santos, Raquel G.; Piro, Oscar Enrique; Castellano, Eduardo E.; Rocha, Willian R.; Beraldo, Heloisa
Año de publicación
2012
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
2-Acetylpyridine-phenylhydrazone (H2AcPh), its para-chlorophenylhydrazone (H2AcpClPh) and paranitrophenylhydrazone (H2AcpNO2Ph) analogues, the corresponding 2-benzoylpyridine-derived hydrazones (H2BzPh, H2BzpClPh and H2BzpNO2Ph) and their gallium(III) complexes were assayed for their cytotoxic activity against U87 (expressing wild-type p53 protein) and T98 (expressing mutant p53 protein) glioma cells. IC50 values against both glioma cells and against the MRC5 (human fetal lung fibroblast) lineage were obtained for the hydrazones, but not for their gallium(III) complexes, due to their low solubility. Hydrazones were highly cytotoxic at nanomolar doses against U87 and T98 cells. The therapeutic indexes (TI ¼ IC50MRC5/IC50glioma) were 2-660 for T98 cells and 28-5000 for U87 cells, indicating that the studied hydrazones could be good antitumor drug candidates to treat brain tumors.
Fil: Despaigne, Angel A. R.. Universidade Federal de Minas Gerais; Brasil
Fil: Parrilha, Gabrieli L.. Universidade Federal de Minas Gerais; Brasil
Fil: Izidoro, Jans B.. Centro de Desenvolvimento Da Tecnologia Nuclear; Brasil
Fil: da Costa, Pryscila R.. Centro de Desenvolvimento Da Tecnologia Nuclear; Brasil
Fil: dos Santos, Raquel G.. Centro de Desenvolvimento Da Tecnologia Nuclear; Brasil
Fil: Piro, Oscar Enrique. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Física La Plata. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Física La Plata; Argentina
Fil: Castellano, Eduardo E.. Universidade de Sao Paulo; Brasil
Fil: Rocha, Willian R.. Universidade Federal de Minas Gerais; Brasil
Fil: Beraldo, Heloisa. Universidade Federal de Minas Gerais; Brasil
Materia
HYDRAZONES
GALLIUM(III) COMPLEXES
CRYSTAL STRUCTURES
GLIOMA CELLS
CYTOTOXIC ACTIVITY
SAR STUDIES
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/268696
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/268696
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cellsDespaigne, Angel A. R.Parrilha, Gabrieli L.Izidoro, Jans B.da Costa, Pryscila R.dos Santos, Raquel G.Piro, Oscar EnriqueCastellano, Eduardo E.Rocha, Willian R.Beraldo, HeloisaHYDRAZONESGALLIUM(III) COMPLEXESCRYSTAL STRUCTURESGLIOMA CELLSCYTOTOXIC ACTIVITYSAR STUDIEShttps://purl.org/becyt/ford/1.7https://purl.org/becyt/ford/12-Acetylpyridine-phenylhydrazone (H2AcPh), its para-chlorophenylhydrazone (H2AcpClPh) and paranitrophenylhydrazone (H2AcpNO2Ph) analogues, the corresponding 2-benzoylpyridine-derived hydrazones (H2BzPh, H2BzpClPh and H2BzpNO2Ph) and their gallium(III) complexes were assayed for their cytotoxic activity against U87 (expressing wild-type p53 protein) and T98 (expressing mutant p53 protein) glioma cells. IC50 values against both glioma cells and against the MRC5 (human fetal lung fibroblast) lineage were obtained for the hydrazones, but not for their gallium(III) complexes, due to their low solubility. Hydrazones were highly cytotoxic at nanomolar doses against U87 and T98 cells. The therapeutic indexes (TI ¼ IC50MRC5/IC50glioma) were 2-660 for T98 cells and 28-5000 for U87 cells, indicating that the studied hydrazones could be good antitumor drug candidates to treat brain tumors.Fil: Despaigne, Angel A. R.. Universidade Federal de Minas Gerais; BrasilFil: Parrilha, Gabrieli L.. Universidade Federal de Minas Gerais; BrasilFil: Izidoro, Jans B.. Centro de Desenvolvimento Da Tecnologia Nuclear; BrasilFil: da Costa, Pryscila R.. Centro de Desenvolvimento Da Tecnologia Nuclear; BrasilFil: dos Santos, Raquel G.. Centro de Desenvolvimento Da Tecnologia Nuclear; BrasilFil: Piro, Oscar Enrique. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Física La Plata. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Física La Plata; ArgentinaFil: Castellano, Eduardo E.. Universidade de Sao Paulo; BrasilFil: Rocha, Willian R.. Universidade Federal de Minas Gerais; BrasilFil: Beraldo, Heloisa. Universidade Federal de Minas Gerais; BrasilElsevier France-Editions Scientifiques Medicales Elsevier2012-04info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/268696Despaigne, Angel A. R.; Parrilha, Gabrieli L.; Izidoro, Jans B.; da Costa, Pryscila R.; dos Santos, Raquel G.; et al.; 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells; Elsevier France-Editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 50; 4-2012; 163-1720223-5234CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0223523412000670info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejmech.2012.01.051info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-22T12:05:30Zoai:ri.conicet.gov.ar:11336/268696instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-10-22 12:05:30.612CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
title 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
spellingShingle 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
Despaigne, Angel A. R.
HYDRAZONES
GALLIUM(III) COMPLEXES
CRYSTAL STRUCTURES
GLIOMA CELLS
CYTOTOXIC ACTIVITY
SAR STUDIES
title_short 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
title_full 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
title_fullStr 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
title_full_unstemmed 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
title_sort 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells
dc.creator.none.fl_str_mv Despaigne, Angel A. R.
Parrilha, Gabrieli L.
Izidoro, Jans B.
da Costa, Pryscila R.
dos Santos, Raquel G.
Piro, Oscar Enrique
Castellano, Eduardo E.
Rocha, Willian R.
Beraldo, Heloisa
author Despaigne, Angel A. R.
author_facet Despaigne, Angel A. R.
Parrilha, Gabrieli L.
Izidoro, Jans B.
da Costa, Pryscila R.
dos Santos, Raquel G.
Piro, Oscar Enrique
Castellano, Eduardo E.
Rocha, Willian R.
Beraldo, Heloisa
author_role author
author2 Parrilha, Gabrieli L.
Izidoro, Jans B.
da Costa, Pryscila R.
dos Santos, Raquel G.
Piro, Oscar Enrique
Castellano, Eduardo E.
Rocha, Willian R.
Beraldo, Heloisa
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv HYDRAZONES
GALLIUM(III) COMPLEXES
CRYSTAL STRUCTURES
GLIOMA CELLS
CYTOTOXIC ACTIVITY
SAR STUDIES
topic HYDRAZONES
GALLIUM(III) COMPLEXES
CRYSTAL STRUCTURES
GLIOMA CELLS
CYTOTOXIC ACTIVITY
SAR STUDIES
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.7
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv 2-Acetylpyridine-phenylhydrazone (H2AcPh), its para-chlorophenylhydrazone (H2AcpClPh) and paranitrophenylhydrazone (H2AcpNO2Ph) analogues, the corresponding 2-benzoylpyridine-derived hydrazones (H2BzPh, H2BzpClPh and H2BzpNO2Ph) and their gallium(III) complexes were assayed for their cytotoxic activity against U87 (expressing wild-type p53 protein) and T98 (expressing mutant p53 protein) glioma cells. IC50 values against both glioma cells and against the MRC5 (human fetal lung fibroblast) lineage were obtained for the hydrazones, but not for their gallium(III) complexes, due to their low solubility. Hydrazones were highly cytotoxic at nanomolar doses against U87 and T98 cells. The therapeutic indexes (TI ¼ IC50MRC5/IC50glioma) were 2-660 for T98 cells and 28-5000 for U87 cells, indicating that the studied hydrazones could be good antitumor drug candidates to treat brain tumors.
Fil: Despaigne, Angel A. R.. Universidade Federal de Minas Gerais; Brasil
Fil: Parrilha, Gabrieli L.. Universidade Federal de Minas Gerais; Brasil
Fil: Izidoro, Jans B.. Centro de Desenvolvimento Da Tecnologia Nuclear; Brasil
Fil: da Costa, Pryscila R.. Centro de Desenvolvimento Da Tecnologia Nuclear; Brasil
Fil: dos Santos, Raquel G.. Centro de Desenvolvimento Da Tecnologia Nuclear; Brasil
Fil: Piro, Oscar Enrique. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Física La Plata. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Física La Plata; Argentina
Fil: Castellano, Eduardo E.. Universidade de Sao Paulo; Brasil
Fil: Rocha, Willian R.. Universidade Federal de Minas Gerais; Brasil
Fil: Beraldo, Heloisa. Universidade Federal de Minas Gerais; Brasil
description 2-Acetylpyridine-phenylhydrazone (H2AcPh), its para-chlorophenylhydrazone (H2AcpClPh) and paranitrophenylhydrazone (H2AcpNO2Ph) analogues, the corresponding 2-benzoylpyridine-derived hydrazones (H2BzPh, H2BzpClPh and H2BzpNO2Ph) and their gallium(III) complexes were assayed for their cytotoxic activity against U87 (expressing wild-type p53 protein) and T98 (expressing mutant p53 protein) glioma cells. IC50 values against both glioma cells and against the MRC5 (human fetal lung fibroblast) lineage were obtained for the hydrazones, but not for their gallium(III) complexes, due to their low solubility. Hydrazones were highly cytotoxic at nanomolar doses against U87 and T98 cells. The therapeutic indexes (TI ¼ IC50MRC5/IC50glioma) were 2-660 for T98 cells and 28-5000 for U87 cells, indicating that the studied hydrazones could be good antitumor drug candidates to treat brain tumors.
publishDate 2012
dc.date.none.fl_str_mv 2012-04
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/268696
Despaigne, Angel A. R.; Parrilha, Gabrieli L.; Izidoro, Jans B.; da Costa, Pryscila R.; dos Santos, Raquel G.; et al.; 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells; Elsevier France-Editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 50; 4-2012; 163-172
0223-5234
CONICET Digital
CONICET
url http://hdl.handle.net/11336/268696
identifier_str_mv Despaigne, Angel A. R.; Parrilha, Gabrieli L.; Izidoro, Jans B.; da Costa, Pryscila R.; dos Santos, Raquel G.; et al.; 2-Acetylpyridine- and 2-benzoylpyridine-derived hydrazones and their gallium(III) complexes are highly cytotoxic to glioma cells; Elsevier France-Editions Scientifiques Medicales Elsevier; European Journal of Medical Chemistry; 50; 4-2012; 163-172
0223-5234
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0223523412000670
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejmech.2012.01.051
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier France-Editions Scientifiques Medicales Elsevier
publisher.none.fl_str_mv Elsevier France-Editions Scientifiques Medicales Elsevier
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 12.982451

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