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dc.contributor.author
Cipriani, Angelo
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dc.contributor.author
Rostán, Santiago
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Leon, Ignacio Esteban
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dc.contributor.author
Li, Zhu Hong
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Gancheff, Jorge S.
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Kemmerling, Ulrike
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Olea Azar, Claudio
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Etcheverry, Susana Beatriz
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Docampo, Roberto
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Gambino, Dinorah
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Otero, Lucía
dc.date.available
2021-10-15T16:09:31Z
dc.date.issued
2020-05
dc.identifier.citation
Cipriani, Angelo; Rostán, Santiago; Leon, Ignacio Esteban; Li, Zhu Hong; Gancheff, Jorge S.; et al.; Multi-target heteroleptic palladium bisphosphonate complexes; Springer Verlag Berlín; Journal of Biological Inorganic Chemistry; 25; 3; 5-2020; 509-519
dc.identifier.issn
0949-8257
dc.identifier.uri
http://hdl.handle.net/11336/143863
dc.description.abstract
Abstract: Bisphosphonates are the most commonly prescribed drugs for the treatment of osteoporosis and other bone illnesses. Some of them have also shown antiparasitic activity. In search of improving the pharmacological profile of commercial bisphosphonates, our group had previously developed first row transition metal complexes with N-containing bisphosphonates (NBPs). In this work, we extended our studies to heteroleptic palladium–NBP complexes including DNA intercalating polypyridyl co-ligands (NN) with the aim of obtaining potential multi-target species. Complexes of the formula [Pd(NBP)2(NN)]·2NaCl·xH2O with NBP = alendronate (ale) or pamidronate (pam) and NN = 1,10 phenanthroline (phen) or 2,2′-bipyridine (bpy) were synthesized and fully characterized. All the obtained compounds were much more active in vitro against T. cruzi (amastigote form) than the corresponding NBP ligands. In addition, complexes were nontoxic to mammalian cells up to 50–100 µM. Compounds with phen as ligand were 15 times more active than their bpy analogous. Related to the potential mechanism of action, all complexes were potent inhibitors of two parasitic enzymes of the isoprenoid biosynthetic pathway. No correlation between the anti-T. cruzi activity and the enzymatic inhibition results was observed. On the contrary, the high antiparasitic activity of phen-containing complexes could be related to their ability to interact with DNA in an intercalative-like mode. These rationally designed compounds are good candidates for further studies and good leaders for future drug developments. Graphic abstract: Four new palladium heteroleptic complexes with N-containing commercial bisphosphonates and DNA intercalating polypyridyl co-ligands were synthesized and fully characterized. All complexes displayed high anti-T. cruzi activity which could be related to the inhibition of the parasitic farnesyl diphosphate synthase enzyme but mainly to their ability to interact DNA. [Figure not available: see fulltext.].
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Springer Verlag Berlín
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
BISPHOSPHONATE
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CHAGAS
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DNA
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PALLADIUM
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TOXOPLASMOSIS
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Química Inorgánica y Nuclear
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dc.subject.classification
Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
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dc.title
Multi-target heteroleptic palladium bisphosphonate complexes
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2021-08-20T19:57:30Z
dc.identifier.eissn
1432-1327
dc.journal.volume
25
dc.journal.number
3
dc.journal.pagination
509-519
dc.journal.pais
Alemania
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dc.journal.ciudad
Berlin
dc.description.fil
Fil: Cipriani, Angelo. Universidad de la República. Facultad de Química; Uruguay
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Fil: Rostán, Santiago. Universidad de la República. Facultad de Química; Uruguay
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Fil: Leon, Ignacio Esteban. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Química Inorgánica "Dr. Pedro J. Aymonino". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Química Inorgánica "Dr. Pedro J. Aymonino"; Argentina
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Fil: Li, Zhu Hong. University Of Georgia. Department Of Cellular Biology; Estados Unidos
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Fil: Gancheff, Jorge S.. Universidad de la República. Facultad de Química; Uruguay
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Fil: Kemmerling, Ulrike. Universidad de Chile. Facultad de Medicina.; Chile
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Fil: Olea Azar, Claudio. Universidad de Chile; Chile
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Fil: Etcheverry, Susana Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Química Inorgánica "Dr. Pedro J. Aymonino". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Química Inorgánica "Dr. Pedro J. Aymonino"; Argentina
dc.description.fil
Fil: Docampo, Roberto. University Of Georgia. Department Of Cellular Biology; Estados Unidos
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Fil: Gambino, Dinorah. Universidad de la República. Facultad de Química; Uruguay
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Fil: Otero, Lucía. Universidad de la República. Facultad de Química; Uruguay
dc.journal.title
Journal of Biological Inorganic Chemistry
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://link.springer.com/10.1007/s00775-020-01779-y
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info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1007/s00775-020-01779-y
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