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.

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, MAY 1 2016. (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, JAN 5 2019. (12/15486-3, 16/17711-5, 14/11340-0)