Advanced search
Start date
Betweenand

NEW Pd(II) ORGANOMETALLIC COMPLEXES: INVESTIGATION OF THEIR POTENTIAL AS CATHEPSIN B INHIBITORS

Grant number: 14/11340-0
Support Opportunities:Scholarships in Brazil - Post-Doctoral
Start date: September 01, 2014
End date: December 10, 2015
Field of knowledge:Physical Sciences and Mathematics - Chemistry - Inorganic Chemistry
Principal Investigator:Adelino Vieira de Godoy Netto
Grantee:Carolina Valério Barra Rocha
Host Institution: Instituto de Química (IQ). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

This project deals with the synthesis, characterization and evaluation of cathepsin B inhibitory activity, involving chelated compounds of the type [{Pd(N C)X}(PR3)] {N C = C2,N-bzox, C2,N-mbz, C2,N-bzan (bzox=benzaldehydeoxime, mbz = N-benzylidenemethylamine, bzan = N-Benzylideneaniline); X = Cl or dmf; (PR3) = triphenylphosphine (PPh3), tricyclohexylphosphine (PCy3), tris(p-tolyl)phosphine (tptp), tris(4-fluorophenyl)phosphine (tfpp)}. The compounds will be characterized by elemental analysis, IR and NMR spectroscopies, ESI/MS mass spectrometry, thermogravimetry (TG) and single crystal X-ray diffraction methods. The stability of compounds under physilogical conditions will be verified by UV-Vis spectroscopy. The potency of inhibition of cathepsin B activity of the ciclometallated complexes will be assayed by fluorometirc experiments. The citotoxicity of compounds towards metastatic, non-metastatic and normal cell lines will be determined by M.T.T. assay. Verification of apoptosis and influence on the cell growth will be verified by flow citometry.For the lipophilicity determination, the new complexes will be submitted to an octanol/water partition and Pd(II) content will be determined in the aquous phase by atomic absorption spectroscopy.

News published in Agência FAPESP Newsletter about the scholarship:
More itemsLess items
Articles published in other media outlets ( ):
More itemsLess items
VEICULO: TITULO (DATA)
VEICULO: TITULO (DATA)

Scientific publications
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
BARRA, CAROLINA V.; ROCHA, FILLIPE V.; MOREL, LAURENT; GAUTIER, ARNAUD; GARRIDO, SAULO S.; MAURO, ANTONIO E.; FREM, REGINA C. G.; NETTO, ADELINO V. G.. DNA binding, topoisomerase inhibition and cytotoxicity of palladium(II) complexes with 1,10-phenanthroline and thioureas. Inorganica Chimica Acta, v. 446, p. 54-60, . (14/11340-0)
BOZZA, GABRIELA F.; DE FARIAS, RENAN L.; DE SOUZA, RONAN F. F.; ROCHA, V, FILLIPE; BARRA, V, CAROLINA; DEFLON, VICTOR M.; DE ALMEIDA, EDUARDO T.; MAURO, ANTONIO E.; NETTO, ADELINO V. G.. Palladium orthometallated complexes containing acetophenoneoxime: Synthesis, crystal structures and hirshfeld surface analysis. Journal of Molecular Structure, v. 1175, p. 195-207, . (12/15486-3, 16/17711-5, 14/11340-0)