The crystallography as tool in the help to elucidate the mechanism of action of potential metallodrugs

• Grant number: 14/13691-4
• Support Opportunities: Regular Research Grants
• Start date: September 01, 2014
• End date: August 31, 2016
• Field of knowledge: Physical Sciences and Mathematics - Physics - General Physics
• Principal Investigator: Eduardo Ernesto Castellano
• Grantee: Eduardo Ernesto Castellano
• Host Institution: Instituto de Física de São Carlos (IFSC). Universidade de São Paulo (USP). São Carlos , SP, Brazil
• Associated researchers: Alzir Azevedo Batista

Abstract

The present project aims the application of techniques for determination of structures by X-ray diffraction of monocrystals to study the bonds in complexes with general formulae [PtCl(PPh3)2(N`-(acyl)-N',N'-(di-substituted)thioureas-k2O,S)], cis-[Pd(PPh3)2(N`-(acyl)-N',N'- (di-substituted)thioureas-k2O,S)]PF6, trans-[Ru(PPh3)2(N`-(acyl)-N',N'-(di-substituted) thioureas-k2O,S)(bipy)]PF6. After the synthesis of the complexes with high purity (by Prof. Alzir Azevedo Batista´s group, Inorganic Chemistry Laboratory, UFSCAR), the cytotoxicity of the complexes against breast and prostate cancer cells, by colorimetric MTT method, the results will be compared with those of fibroblast cells, to make the screening for further study with respect the death mecanism of action and the interactions of the complexes with DNA. Knowing the molecular geometry of the complexes, and with the help of other techniques, such as NMR, UV-Vis, IR, there is a expectation to be possible to relate structure and activity of the complexes under study. (AU)

Scientific publications

(4)

(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)

PLUTIN, ANA M.; ALVAREZ, ANISLAY; MOCELO, RAUL; RAMOS, RAUL; CASTELLANO, EDUARDO E.; DA SILVA, MONIZE M.; COLINA-VEGAS, LEGNA; PAVAN, FERNANDO R.; BATISTA, ALZIR A.. Anti-Mycobacterium tuberculosis activity of platinum(II)/N,N-disubstituted-N `-acyl thiourea complexes. Inorganic Chemistry Communications, v. 63, p. 74-80, JAN 2016. (14/13691-4, 13/14957-5)

PLUTIN, ANA M.; ALVAREZ, ANISLAY; MOCELO, RAUL; RAMOS, RAUL; CASTELLANO, EDUARDO E.; DA SILVA, MONIZE M.; VILLARREAL, WILMER; PAVAN, FERNANDO R.; MEIRA, CASSIO SANTANA; RODRIGUES FILHO, JOSE SIMAO; et al. Palladium(II)/N,N-disubstituted-N `-acylthioureas complexes as anti-Mycobacterium tuberculosis and anti-Trypanosoma cruzi agents. Polyhedron, v. 132, p. 70-77, AUG 16 2017. (14/13691-4)

PLUTIN, ANA M.; ALVAREZ, ANISLAY; MOCELO, RAUL; RAMOS, RAUL; CASTELLANO, EDUARDO E.; DA SILVA, MONIZE M.; COLINA-VEGAS, LEGNA; PAVAN, FERNANDO R.; BATISTA, ALZIR A.. Anti-Mycobacterium tuberculosis activity of platinum(II)/N,N-disubstituted-N '-acyl thiourea complexes. Inorganic Chemistry Communications, v. 63, p. 7-pg., 2016-01-01. (13/14957-5, 14/13691-4)

PLUTIN, ANA M.; ALVAREZ, ANISLAY; MOCELO, RAUL; RAMOS, RAUL; CASTELLANO, EDUARDO E.; DA SILVA, MONIZE M.; VILLARREAL, WILMER; PAVAN, FERNANDO R.; MEIRA, CASSIO SANTANA; RODRIGUES FILHO, JOSE SIMAO; et al. Palladium(II)/N,N-disubstituted-N '-acylthioureas complexes as anti-Mycobacterium tuberculosis and anti-Trypanosoma cruzi agents. Polyhedron, v. 132, p. 8-pg., 2017-08-16. (14/13691-4)