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
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/25238
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oai:ri.conicet.gov.ar:11336/25238 |
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CONICET Digital (CONICET) |
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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 Técnicas2025-09-29T09:49:06Zoai: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:34982025-09-29 09:49:07.259CONICET 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 |
_version_ |
1844613522322882560 |
score |
13.070432 |