Four ruthenium(II)-based complexes with N-(acyl)-N',N'-(disubstituted)thiourea derivatives (Th) were obtained. The compounds, with the general formula trans-[Ru(PPh3)2(Th)(bipy)]PF6, interact with bovine serum albumin (BSA) and DNA. BSA-binding constants, which were in the range of 3.3-6.5×10(4) M(-1), and the thermodynamic parameters (ΔG, ΔH and ΔS), suggest spontaneous interactions with this protein by electrostatic forces due to the positive charge of the complexes. Also, binding constant by spectrophotometric DNA titration (Kb = 0.8-1.8×10(4) M(-1)) and viscosity studies indicate weak interactions between the complexes and DNA. Cytotoxicity assays against DU-145 (prostate cancer) and A549 (lung cancer) tumour cells revealed that the complexes are more active in tumour cells than in normal (L929) cells, and that they present high cytotoxicity (low IC50 values) compared with the reference metallodrug, cisplatin.
Synthesis, characterization and anti-Mycobacterium tuberculosis assays of new platinum(II)/dppf/N,Ndisubstituted-N′-acyl thiourea complexes with general formulae [Pt(dppf)(L)]PF 6 , [dppf = 1,1′-bis (diphenylphosphino)ferrocene; L = N,N-disubstituted-N′-acyl thioureas] is reported. The complexes were characterized by elemental analysis, molar conductivity, IR, NMR (1 H, 13 C and 31 P{ 1 H}) spectroscopy. The spectroscopic data are consistent with the complexes containing one dppf and one O, S chelated ligand. The crystal structures of complexes with N,N-diphenyl-N′-benzoylthiourea (L4), N,N-diethyl-N′-furoylthiourea (L5) and N,N-diphenyl-N′-(thiophene-2-carbonyl)thiourea (L8) were determined by X-ray crystallography, confirming the coordination of the ligands with the metal through sulfur and oxygen atoms, forming distorted square-planar structures. The complexes were screened with respect to their anti-M. tuberculosis activity (H37Rv ATCC 27294).
In the title compound, C10H12N2OS, the amide NCO group is twisted relative to the thioureido SCN2 group, forming a dihedral angle of 55.3 (2)°. The crystal packing shows intermolecular N—H⋯S and weak C—H⋯O interactions, the former giving rise to the formation of centrosymmetric R
2
2(8) dimers.
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