Show simple item record

Authordc.contributor.authorRodríguez Arce, Esteban 
Authordc.contributor.authorPutzu, Eugenia 
Authordc.contributor.authorLapier, Michel 
Authordc.contributor.authorMaya Arango, Juan 
Authordc.contributor.authorOlea Azar, Claudio
Authordc.contributor.authorEcheverría, Gustavo A. 
Authordc.contributor.authorPiro, Oscar E. 
Authordc.contributor.authorMedeiros, Andrea 
Authordc.contributor.authorSardi, Florencia 
Authordc.contributor.authorComini, Marcelo 
Authordc.contributor.authorRisi, Gastón 
Authordc.contributor.authorSalinas, Gustavo 
Authordc.contributor.authorCorreia, Isabel 
Authordc.contributor.authorPessoa, João Costa 
Authordc.contributor.authorOtero, Lucía 
Cita de ítemdc.identifier.citationDalton Transactions, Volumen 48, Issue 22, 2019, Pages 7644-7658
Abstractdc.description.abstractIn the search for a more effective chemotherapy for the treatment of Chagas' disease and human African trypanosomiasis, caused by Trypanosoma cruzi and Trypanosoma brucei parasites, respectively, the use of organometallic compounds may be a promising strategy. In this work, eight new heterobimetallic compounds are described including four 5-nitrofuryl containing thiosemicarbazones as bioactive ligands (HL1-HL4) and dppf = 1,1′-bis(diphenylphosphino) ferrocene as an organometallic co-ligand. Complexes of the formula [MII(L)(dppf)](PF6) with M = Pd or Pt were synthesized and fully characterized in the solid state and in solution, including the determination of the molecular structure of four of them by single crystal X-ray diffraction methods. Most compounds showed activity in the low micromolar or submicromolar range against both parasites, with the platinum compounds being more active than the palladium analogues. Activity was significantly increased by generation of the M-dppf compounds (3-24 fold increase with respect to free ligands HL for T. cruzi and up to 99 fold increase with respect to HL for T. brucei). The inclusion of the organometallic co-ligand also led to lower toxicity in mammalian cells and higher selectivity towards both parasites when compared to the free HL compounds. The complexes interact with DNA and affect the redox metabolism of the parasites. Furthermore, the most active and selective compound of the new series showed no in vivo toxicity in zebrafish embryos.
Publisherdc.publisherRoyal Society of Chemistry
Type of licensedc.rightsAttribution-NonCommercial-NoDerivs 3.0 Chile
Link to Licensedc.rights.uri
Sourcedc.sourceDalton Transactions
Keywordsdc.subjectInorganic Chemistry
Títulodc.titleNew heterobimetallic ferrocenyl derivatives are promising antitrypanosomal agents
Document typedc.typeArtículo de revista
dcterms.accessRightsdcterms.accessRightsAcceso Abierto
Indexationuchile.indexArtículo de publicación SCOPUS

Files in this item


This item appears in the following Collection(s)

Show simple item record

Attribution-NonCommercial-NoDerivs 3.0 Chile
Except where otherwise noted, this item's license is described as Attribution-NonCommercial-NoDerivs 3.0 Chile