Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective an...

Autores
Gomez, Natalia; Santos, Diego; Vazquez, Ramiro; Suescun, Leopoldo; Mombru, Alvaro; Vermeulen, Elba Monica; Finkielsztein, Liliana Mónica; Shayo, Carina Claudia; Moglioni, Albertina Gladys; Gambino, Dinorah; Davio, Carlos Alberto
Año de publicación
2011
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
In the search for alternative chemotherapeutic strategies against leukemia, various 1-indanone thiosemicarbazones, as well as eight novel platinum(II) and palladium(II) complexes, with the formula [MCl2(HL)] and [M(HL)(L)]Cl, derived from two 1-indanone thiosemicarbazones were synthesized and tested for antiproliferative activity against the human leukemia U937 cell line. The crystal structure of [Pt(HL1)(L1)]Cl.2MeOH, where L1=1-indanone thiosemicarbazone, was solved by X-ray diffraction. Free thiosemicarbazone ligands showed no antiproliferative effect, but the corresponding platinum(II) and palladium( II) complexes inhibited cell proliferation and induced apoptosis. Platinum(II) complexes also displayed selective apoptotic activity in U937 cells but not in peripheral blood monocytes or the human hepatocellular carcinoma HepG2 cell line used to screen for potential hepatotoxicity. Present findings show that, in U937 cells, 1-indanone thiosemicarbazones coordinated to palladium(II) were more cytotoxic than those complexed with platinum(II), although the latter were found to be more selective for leukemic cells suggesting that they are promising compounds with potential therapeutic application against hematological malignancies.
Fil: Gomez, Natalia. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Santos, Diego. Universidad de la República; Uruguay
Fil: Vazquez, Ramiro. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Suescun, Leopoldo. Universidad de la República; Uruguay
Fil: Mombru, Alvaro. Universidad de la República; Uruguay
Fil: Vermeulen, Elba Monica. Academia Nacional de Medicina de Buenos Aires; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Finkielsztein, Liliana Mónica. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina
Fil: Shayo, Carina Claudia. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Moglioni, Albertina Gladys. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Gambino, Dinorah. Universidad de la República; Uruguay
Fil: Davio, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Materia
Apoptosis
Drug Discovery
Leukemia
Thiosemicarbazones
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:11336/25238
Acceder
id CONICETDig_59a5dcaf560af0f0dd114ed178668525
oai_identifier_str oai:ri.conicet.gov.ar:11336/25238
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agentsGomez, NataliaSantos, DiegoVazquez, RamiroSuescun, LeopoldoMombru, AlvaroVermeulen, Elba MonicaFinkielsztein, Liliana MónicaShayo, Carina ClaudiaMoglioni, Albertina GladysGambino, DinorahDavio, Carlos AlbertoApoptosisDrug DiscoveryLeukemiaThiosemicarbazoneshttps://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/3https://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/3In the search for alternative chemotherapeutic strategies against leukemia, various 1-indanone thiosemicarbazones, as well as eight novel platinum(II) and palladium(II) complexes, with the formula [MCl2(HL)] and [M(HL)(L)]Cl, derived from two 1-indanone thiosemicarbazones were synthesized and tested for antiproliferative activity against the human leukemia U937 cell line. The crystal structure of [Pt(HL1)(L1)]Cl.2MeOH, where L1=1-indanone thiosemicarbazone, was solved by X-ray diffraction. Free thiosemicarbazone ligands showed no antiproliferative effect, but the corresponding platinum(II) and palladium( II) complexes inhibited cell proliferation and induced apoptosis. Platinum(II) complexes also displayed selective apoptotic activity in U937 cells but not in peripheral blood monocytes or the human hepatocellular carcinoma HepG2 cell line used to screen for potential hepatotoxicity. Present findings show that, in U937 cells, 1-indanone thiosemicarbazones coordinated to palladium(II) were more cytotoxic than those complexed with platinum(II), although the latter were found to be more selective for leukemic cells suggesting that they are promising compounds with potential therapeutic application against hematological malignancies.Fil: Gomez, Natalia. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Santos, Diego. Universidad de la República; UruguayFil: Vazquez, Ramiro. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Suescun, Leopoldo. Universidad de la República; UruguayFil: Mombru, Alvaro. Universidad de la República; UruguayFil: Vermeulen, Elba Monica. Academia Nacional de Medicina de Buenos Aires; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Finkielsztein, Liliana Mónica. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; ArgentinaFil: Shayo, Carina Claudia. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Moglioni, Albertina Gladys. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Gambino, Dinorah. Universidad de la República; UruguayFil: Davio, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaWiley VCH Verlag2011info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/25238Gomez, Natalia; Santos, Diego; Vazquez, Ramiro; Suescun, Leopoldo; Mombru, Alvaro; et al.; Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents; Wiley VCH Verlag; Chemmedchem; 6; 8; -1-2011; 1485-14941860-71791860-7187CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201100060info:eu-repo/semantics/altIdentifier/doi/10.1002/cmdc.201100060info:eu-repo/semantics/altIdentifier/pmid/21608131info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-15T14:43:10Zoai:ri.conicet.gov.ar:11336/25238instacron: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:34982025-10-15 14:43:10.339CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
title Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
spellingShingle Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
Gomez, Natalia
Apoptosis
Drug Discovery
Leukemia
Thiosemicarbazones
title_short Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
title_full Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
title_fullStr Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
title_full_unstemmed Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
title_sort Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents
dc.creator.none.fl_str_mv Gomez, Natalia
Santos, Diego
Vazquez, Ramiro
Suescun, Leopoldo
Mombru, Alvaro
Vermeulen, Elba Monica
Finkielsztein, Liliana Mónica
Shayo, Carina Claudia
Moglioni, Albertina Gladys
Gambino, Dinorah
Davio, Carlos Alberto
author Gomez, Natalia
author_facet Gomez, Natalia
Santos, Diego
Vazquez, Ramiro
Suescun, Leopoldo
Mombru, Alvaro
Vermeulen, Elba Monica
Finkielsztein, Liliana Mónica
Shayo, Carina Claudia
Moglioni, Albertina Gladys
Gambino, Dinorah
Davio, Carlos Alberto
author_role author
author2 Santos, Diego
Vazquez, Ramiro
Suescun, Leopoldo
Mombru, Alvaro
Vermeulen, Elba Monica
Finkielsztein, Liliana Mónica
Shayo, Carina Claudia
Moglioni, Albertina Gladys
Gambino, Dinorah
Davio, Carlos Alberto
author2_role author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Apoptosis
Drug Discovery
Leukemia
Thiosemicarbazones
topic Apoptosis
Drug Discovery
Leukemia
Thiosemicarbazones
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.1
https://purl.org/becyt/ford/3
https://purl.org/becyt/ford/3.1
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv In the search for alternative chemotherapeutic strategies against leukemia, various 1-indanone thiosemicarbazones, as well as eight novel platinum(II) and palladium(II) complexes, with the formula [MCl2(HL)] and [M(HL)(L)]Cl, derived from two 1-indanone thiosemicarbazones were synthesized and tested for antiproliferative activity against the human leukemia U937 cell line. The crystal structure of [Pt(HL1)(L1)]Cl.2MeOH, where L1=1-indanone thiosemicarbazone, was solved by X-ray diffraction. Free thiosemicarbazone ligands showed no antiproliferative effect, but the corresponding platinum(II) and palladium( II) complexes inhibited cell proliferation and induced apoptosis. Platinum(II) complexes also displayed selective apoptotic activity in U937 cells but not in peripheral blood monocytes or the human hepatocellular carcinoma HepG2 cell line used to screen for potential hepatotoxicity. Present findings show that, in U937 cells, 1-indanone thiosemicarbazones coordinated to palladium(II) were more cytotoxic than those complexed with platinum(II), although the latter were found to be more selective for leukemic cells suggesting that they are promising compounds with potential therapeutic application against hematological malignancies.
Fil: Gomez, Natalia. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Santos, Diego. Universidad de la República; Uruguay
Fil: Vazquez, Ramiro. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Suescun, Leopoldo. Universidad de la República; Uruguay
Fil: Mombru, Alvaro. Universidad de la República; Uruguay
Fil: Vermeulen, Elba Monica. Academia Nacional de Medicina de Buenos Aires; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Finkielsztein, Liliana Mónica. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina
Fil: Shayo, Carina Claudia. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Moglioni, Albertina Gladys. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Gambino, Dinorah. Universidad de la República; Uruguay
Fil: Davio, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
description In the search for alternative chemotherapeutic strategies against leukemia, various 1-indanone thiosemicarbazones, as well as eight novel platinum(II) and palladium(II) complexes, with the formula [MCl2(HL)] and [M(HL)(L)]Cl, derived from two 1-indanone thiosemicarbazones were synthesized and tested for antiproliferative activity against the human leukemia U937 cell line. The crystal structure of [Pt(HL1)(L1)]Cl.2MeOH, where L1=1-indanone thiosemicarbazone, was solved by X-ray diffraction. Free thiosemicarbazone ligands showed no antiproliferative effect, but the corresponding platinum(II) and palladium( II) complexes inhibited cell proliferation and induced apoptosis. Platinum(II) complexes also displayed selective apoptotic activity in U937 cells but not in peripheral blood monocytes or the human hepatocellular carcinoma HepG2 cell line used to screen for potential hepatotoxicity. Present findings show that, in U937 cells, 1-indanone thiosemicarbazones coordinated to palladium(II) were more cytotoxic than those complexed with platinum(II), although the latter were found to be more selective for leukemic cells suggesting that they are promising compounds with potential therapeutic application against hematological malignancies.
publishDate 2011
dc.date.none.fl_str_mv 2011
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/11336/25238
Gomez, Natalia; Santos, Diego; Vazquez, Ramiro; Suescun, Leopoldo; Mombru, Alvaro; et al.; Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents; Wiley VCH Verlag; Chemmedchem; 6; 8; -1-2011; 1485-1494
1860-7179
1860-7187
CONICET Digital
CONICET
url http://hdl.handle.net/11336/25238
identifier_str_mv Gomez, Natalia; Santos, Diego; Vazquez, Ramiro; Suescun, Leopoldo; Mombru, Alvaro; et al.; Synthesis, structural characterization and pro-apoptotic activity of Indanone thiosemicarbazones and their platinum (II) and paladium (II) complexes: Potential role as selective antileukemic agents; Wiley VCH Verlag; Chemmedchem; 6; 8; -1-2011; 1485-1494
1860-7179
1860-7187
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://onlinelibrary.wiley.com/doi/10.1002/cmdc.201100060
info:eu-repo/semantics/altIdentifier/doi/10.1002/cmdc.201100060
info:eu-repo/semantics/altIdentifier/pmid/21608131
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
application/pdf
dc.publisher.none.fl_str_mv Wiley VCH Verlag
publisher.none.fl_str_mv Wiley VCH Verlag
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 13.22299

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