http://www.cnr.it/ontology/cnr/individuo/prodotto/ID191877

Activity on Trypanosoma cruzi, erythrocytes lysis and biologically relevant physicochemical properties of Pd(II) and Pt(II) complexes of thiosemicarbazones derived from 1-indanones (Articolo in rivista)

Type

Articolo in rivista (Classe)
Prodotto della ricerca (Classe)

Label

Activity on Trypanosoma cruzi, erythrocytes lysis and biologically relevant physicochemical properties of Pd(II) and Pt(II) complexes of thiosemicarbazones derived from 1-indanones (Articolo in rivista) (literal)

Anno

2012-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

10.1016/j.jinorgbio.2012.08.024 (literal)

Alternative label

Diego Santos, Beatriz Parajón-Costa, Miriam Rossi, Caruso F, Diego Benítez, Javier Varela, Hugo Cerecetto, Mercedes González, Natalia Gómez, María E. Caputto, Albertina G. Moglioni, Graciela Y. Moltrasio, Liliana M. Finkielsztein, Dinorah Gambino (2012)
Activity on Trypanosoma cruzi, erythrocytes lysis and biologically relevant physicochemical properties of Pd(II) and Pt(II) complexes of thiosemicarbazones derived from 1-indanones
in Journal of inorganic biochemistry
(literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

Diego Santos, Beatriz Parajón-Costa, Miriam Rossi, Caruso F, Diego Benítez, Javier Varela, Hugo Cerecetto, Mercedes González, Natalia Gómez, María E. Caputto, Albertina G. Moglioni, Graciela Y. Moltrasio, Liliana M. Finkielsztein, Dinorah Gambino (literal)

Pagina inizio

270 (literal)

Pagina fine

276 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#altreInformazioni

Rerint ottenibile presso l'editore dietro pagamento (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#url

http://dx.doi.org/10.1016/j.jinorgbio.2012.08.024 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

117 (literal)

Rivista

Journal of inorganic biochemistry (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali

7 (literal)

Note

PubMe (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

Cátedra de Química Inorgánica, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay; Centro de Química Inorgánica (CEQUINOR/CONICET-UNLP), C.C. 962, Facultad de Ciencias Exactas, Universidad Nacional de La Plata, 1900 La Plata, Argentina; Department of Chemistry, Vassar College, Poughkeepsie, New York 12604-0484, USA; Istituto di Chimica Biomolecolare, Consiglio Nazionale delle Ricerche, c/o Università di Roma La Sapienza, Vecchio Istituto Chimico, P.le Aldo Moro 5, 00185 Rome, Italy; Grupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias-Facultad de Química, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay; Química Medicinal, Departamento de Farmacología, Universidad de Buenos Aires, Junín 956, 1113 Buenos Aires, Argentina; Departamento de Química Orgánica, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956, 1113 Buenos Aires, Argentina; (literal)

Titolo

Activity on Trypanosoma cruzi, erythrocytes lysis and biologically relevant physicochemical properties of Pd(II) and Pt(II) complexes of thiosemicarbazones derived from 1-indanones (literal)

Abstract

American trypanosomiasis or Chagas disease, caused by the protist parasite Trypanosoma cruzi (T. cruzi), is a major health concern in Latin America. In the search for new bioactive compounds, eight Pd(II) and Pt(II) complexes of thiosemicarbazones derived from 1-indanones (HL) were evaluated as potential anti-T. cruzi compounds. Their unspecific cytotoxicity was determined on human erythrocytes. Two physicochemical features, lipophilicity and redox behavior, that could be potentially relevant for the biological activity of these complexes, were determined. Crystal structure of [Pd(HL1)(L1)]Cl·CH3OH, where HL1=1-indanone thiosemicarbazone, was solved by X-ray diffraction methods. Five of the eight metal complexes showed activity against T. cruzi with IC50 values in the low micromolar range and showed significantly higher activity than the corresponding free ligands. Four of them resulted more active against the parasite than the reference antitrypanosomal drug Nifurtimox. Anti-T. cruzi activity and selectivity towards the parasite were both higher for the Pd(II) compounds than for the Pt(II) analogues, showing the effect of the metal center selection on the biological behavior. Among both physicochemical features tested for this series of compounds, lipophilicity and redox behavior, only the former seemed to show correlation with the antiproliferative effects observed. Metal coordination improved bioactivity but lead to an increase of mammalian cytotoxicity. Nevertheless, some of the metal complexes tested in this work still show suitable selectivity indexes and deserve further developments. (literal)

Prodotto di