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

2008 
Abstract The reaction of cis -[RuCl 2 (dppb)(N–N)], dppb = 1,4-bis(diphenylphosphino)butane, complexes with the ligand HSpymMe 2 , 4,6-dimethyl-2-mercaptopyrimidine, yielded the cationic complexes [Ru(SpymMe 2 )(dppb)(N–N)]PF 6 , 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 -[RuCl 2 (dppb)(N–N)], N–N = bipy ( 3 ) and Me-bipy ( 4 ) and the free ligands dppb, bipy, Me-bipy and SpymMe 2 . The minimal inhibitory concentration (MIC) of compounds needed to kill 90% of mycobacterial cells and the IC 50 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 IC 50 values of 0.46 ± 0.02 and 0.43 ± 0.08 μM, respectively, against MDA-MB-231 breast tumor cells.
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