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
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/268696
Ver los metadatos del registro completo
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3498 |
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CONICET Digital (CONICET) |
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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 Técnicas2025-09-29T10:32:58Zoai: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:34982025-09-29 10:32:59.045CONICET 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 |
_version_ |
1844614344410660864 |
score |
13.070432 |