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A new series of mononuclear ruthenium(II) complexes of the type [Ru(PPh3)2(N,S-L1–3)2] 2H3O+.(Cl−)2.XH2O, [RuCl(dmso)3(N,S-L1–3)], and [Ru2(Cl−)2(N,S-L1–3)2].XH2O, where L1 is ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-pyrimidine-5-carboxylate (monastrol), and L2 and L3 are the 4-hydroxyphenyl and 4-bromophenyl analogs of monastrol have been prepared and characterized by elemental analysis, 1H, and 13C 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-L1)] (7) and [RuCl(dmso)3(N,S-L2)] (8) showed cytotoxicity values of > 0.21 and > 2.14 µM, respectively against mock-infected MT-4 cells. In addition, complexes [Ru(PPh3)2(N,S-L3)2].2H3O+.2Cl−.H2O (4), 7, and [RuCl2(N,S-L1)] (10) have been selected for evaluation of their dual inhibition activity against dual-specificity tyrosine phosphorylation-regulated kinase (Dyrk1A). [ABSTRACT FROM AUTHOR]

Three new ruthenium(II)-arene complexes of the general formula [{(η6-p-cymene)Ru(L)}2](Cl)2), where L are monastrol (L1), ethyl 4-(3-hydroxyphenyl)-6-methyl-2-thioxo-pyrimidine-5-carboxylate (L2) or its 4-bromophenyl analog (L3), have been synthesized and characterized by elemental analysis, 1H, 13C, and 2-D NMR spectroscopy. The X-ray diffraction study of complex 1 showed the presence of a dicationic diruthenium complex where two thioxopyrimidines act as tridentate μ,κN:κ2S ligand, bridging two Ru ions through the pyrimidine nitrogen and sulfur atoms. All new complexes were evaluated in vitro for their antiviral activity against the replication of HIV-1 and HIV-2 in MT-4 cells using MTT assay. Additionally, complexes 1–3 were screened for their inhibitory activity against the ATPase enzyme and the motor-protein Kinesin Eg5. Complex 1 was found to inhibit microtubule-stimulated ATPase activity of kinesin of IC50 = 30 μM (monastrol, IC50 = 10 μM). [ABSTRACT FROM AUTHOR]