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Synthesis, characterization, X-ray structure and in vitro antimycobacterial and antitumoral activities of Ru(II) phosphine/diimine complexes containing the "SpymMe2" ligand, SpymMe2=4,6-dimethyl-2-mercaptopyrimidine |
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| Authors: | do Nascimento Fábio B Von Poelhsitz Gustavo Pavan Fernando R Sato Daisy N Leite Clarice Q F Selistre-de-Araújo Heloisa S Ellena Javier Castellano Eduardo E Deflon Victor M Batista Alzir A |
| Affiliation: | a Departamento de Química, Universidade Federal de São Carlos, CP 676, CEP 13565-905, São Carlos, SP, Brazil b Departamento de Química, Campus Catalão, Universidade Federal de Goiás, CP 56, CEP 75704-020, Catalão, GO, Brazil c Departamento de Ciências Biológicas, Faculdade de Ciências Farmacêuticas, UNESP, CEP 14800-900, Araraquara, SP, Brazil d Instituto Adolfo Lutz, Laboratório de Ribeirão Preto, CEP 14085-410, Ribeirão Preto, SP, Brazil e Departamento de Ciências Fisiológicas, Universidade Federal de São Carlos, CP 676, CEP 13565-905, São Carlos, SP, Brazil f Instituto de Física de São Carlos, Universidade de São Paulo, CP 369, CEP 13560-970, São Carlos, SP, Brazil g Instituto de Química de São Carlos, Universidade de São Paulo, CP 780, CEP 13560-970, São Carlos, SP, Brazil |
| Abstract: | The reaction of cis-[RuCl2(dppb)(N-N)], dppb = 1,4-bis(diphenylphosphino)butane, complexes with the ligand HSpymMe2, 4,6-dimethyl-2-mercaptopyrimidine, yielded the cationic complexes [Ru(SpymMe2)(dppb)(N-N)]PF6, N-N = bipy (1) and Me-bipy (2), bipy = 2,2′-bipyridine and Me-bipy = 4,4′-dimethyl-2,2′-bipyridine, which were characterized by spectroscopic and electrochemical techniques and X-ray crystallography and elemental analysis. Additionally, preliminary in vitro tests for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27264 and antitumor activity against the MDA-MB-231 human breast tumor cell line were carried out on the new complexes and also on the precursors cis-[RuCl2(dppb)(N-N)], N-N = bipy (3) and Me-bipy (4) and the free ligands dppb, bipy, Me-bipy and SpymMe2. The minimal inhibitory concentration (MIC) of compounds needed to kill 90% of mycobacterial cells and the IC50 values for the antitumor activity were determined. Compounds 1-4 exhibited good in vitro activity against M. tuberculosis, with MIC values ranging between 0.78 and 6.25 μg/mL, compared to the free ligands (MIC of 25 to >50 μg/mL) and the drugs used to treat tuberculosis. Complexes 1 and 2 also showed promising antitumor activity, with IC50 values of 0.46 ± 0.02 and 0.43 ± 0.08 μM, respectively, against MDA-MB-231 breast tumor cells. |
| Keywords: | Ruthenium (II) complex Cytotoxicity Antimycobacterial activity dppb 4,6-dimethyl-2-mercaptopyrimidine |
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