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Abstract
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).
Graphical Abstract
Acknowledgements
We thank Prof. C. Pannecouque of Rega Institute for Medical Research, Katholieke Universiteit, Leuven, Belgium, for the anti-HIV screening. W. Al-Masoudi would like to thank Basrah University for the sabbatical leave and Prof. Winter for hosting him at the University of Konstanz. Miss A. Friemel and Mr. U. Haunz, of Chemistry Department, Konstanz University, Germany are acknowledged for the NMR experiments. The authors also thank Dr. M. Engel of Pharmaceutical and Medicial Chemistry, Saarland University, Saarbrüken, Germany, for the inhibition screening of Dyrk1A.