Anti-Mycobacterium tuberculosis and Cytotoxicity Activities of Ruthenium(II)/ Bipyridine/Diphosphine/Pyrimidine-2-thiolate Complexes: The Role of the Non- Coordinated N-Atom

Author(s)

Benedicto A. V. Lima ^[1] ; Rodrigo S. Corrêa ; Angelica E. Graminha ^[3] ; Aleksey Kuznetsov ^[4] ; Javier Ellena ^[5] ; Fernando R. Pavan ^[6] ; Clarice Q. F. Leite ^[7] ; Alzir A. Batista ^[8]

Affiliation

^[1] Universidade Federal de São Carlos. Departamento de Química - Brasil

^[3] Universidade Federal de São Carlos. Departamento de Química - Brasil

^[4] Universidade Federal de São Carlos. Departamento de Química - Brasil

^[5] Universidade de São Paulo. Instituto de Física de São Carlos - Brasil

^[6] Universidade Estadual Paulista. Faculdade de Ciências Farmacêuticas. Departamento de Ciências Biológicas - Brasil

^[7] Universidade Estadual Paulista. Faculdade de Ciências Farmacêuticas. Departamento de Ciências Biológicas - Brasil

^[8] Universidade Federal de São Carlos. Departamento de Química - Brasil

• Document type: Journal article
• Source: Journal of the Brazilian Chemical Society; v. 27, n. 1, p. 30-40, 2016-01-00.

Abstract

The [Ru(Spym)(bipy)(P–P)]PF6, [Spym = pyrimidine-2-thiolate anion; P–P = 1,2-bis(diphenylphosphino)ethane, 1,3-bis(diphenylphosphino)propane and 1,1'-bis(diphenylphosphino)ferrocene] complexes were synthesized and characterized by spectroscopic, electrochemical and elemental analysis, and by X-ray crystallography. The minimal inhibitory concentration (MIC) of the compounds against Mycobacterium tuberculosis and the complex concentration causing 50% tumor cell growth inhibition (IC50) against breast cancer cells, MDA-MB-231, were determined. All three compounds gave promising values in both tests. It is interesting to mention that all three complexes display MICs against Mycobacteriumtuberculosis showing higher activity than cycloserine, a second line drug used in the treatment of the illness. The complexes interact weakly with the DNA. (AU)

• FAPESP's process: 13/26559-4 - Structural modifications in biologically active Ru(II) complexes toward the design of new metallodrug candidates
• Grantee: Rodrigo de Souza Corrêa
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 12/06013-4 - Study of apoptosis gene expression, celular cyclic, DNA repair and oxidative stress in cells of human lang carcinoma treated with complexes with general formula [Ru(AA)(dppb)(bipy)]PF6
• Grantee: Alzir Azevedo Batista
• Support Opportunities: Regular Research Grants