A ruthenium complexes of monastrol and its pyrimidine analogues: Synthesis and biological properties

A new series of mononuclear ruthenium(II) complexes of the type [Ru(PPh3)(2)(N,S-L-1?3)(2)] 2H(3)O(+).(Cl-?)(2.)XH2O, [RuCl(dmso)(3)(N,S-L-1?3)], and [Ru-2(Cl-?)(2)(N,S-L-1?3)(2)].XH2O, where L-1 is ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-pyrimidine-5-carboxylate (monastrol), and L-2 and L-3 are the 4-hydroxyphenyl and 4-bromophenyl analogs of monastrol have been prepared and characterized by elemental analysis, H-1, and C-13 NMR spectroscopy. All the complexes were assayed for their anti-HIV-1 and HIV-2 activity in MT-4 cells, and cytotoxicity was also investigated in mock-infected in MT-4 cells by using MTT assay. All the complexes exhibited no anti-HIV activity, however complexes [RuCl(dmso)(3)(N,S-L-1)] (7) and [RuCl(dmso)(3)(N,S-L-2)] (8) showed cytotoxicity values of > 0.21 and > 2.14 ?M, respectively against mock-infected MT-4 cells. In addition, complexes [Ru(PPh3)(2)(N,S-L-3)(2)].2H(3)O(+).2Cl(?).H2O (4), 7, and [RuCl2(N,S-L-1)] (10) have been selected for evaluation of their dual inhibition activity against dual-specificity tyrosine phosphorylation-regulated kinase (Dyrk1A).