Novel Ru(III) Complexes with Some Benzothiazole Derivatives: Synthesis, Physicochemical and Pharmacological Investigations

A. Nikolova; G. Momekov; A. Bakalova; K. Nikolova; D. Ivanov

doi:10.1055/s-0034-1382052

Drug Research, Inhaltsverzeichnis

Drug Res (Stuttg) 2015; 65(06): 317-322
DOI: 10.1055/s-0034-1382052

Original Article

Novel Ru(III) Complexes with Some Benzothiazole Derivatives: Synthesis, Physicochemical and Pharmacological Investigations

Authors

A. Nikolova

¹Department of Chemistry, Faculty of Pharmacy, Medical University – Sofia, Sofia, Bulgaria
G. Momekov

²Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University – Sofia, Sofia, Bulgaria
A. Bakalova

¹Department of Chemistry, Faculty of Pharmacy, Medical University – Sofia, Sofia, Bulgaria
K. Nikolova

¹Department of Chemistry, Faculty of Pharmacy, Medical University – Sofia, Sofia, Bulgaria
D. Ivanov

¹Department of Chemistry, Faculty of Pharmacy, Medical University – Sofia, Sofia, Bulgaria

Abstract

In this work we present 3 new complexes of Ruthenium (III) with a general formula HL[Ru(L)₂Cl₄], where L=benzothiazole, 2-methylbenzothiazole and 2-mercaptobenzothiazole. The syntheses were carried out in polar medium under argon. The compounds obtained were characterised by IR-, ¹H-NMR- ¹³C-NMR-, UV-VIS-spectroscopy and conductivity measurements. The ligands behaved as monodentate, bounding Ru(III) through the nitrogen atoms from the heterocycle. The cytotoxicity of the new complexes was tested against 2 human leukemic cell lines (K-562 and KE-37), using the MTT-dye reduction assay. The Ru(III) coordination compound with 2-methylbenzothiazole displayed superior activity compared to the other novel complexes. Its IC50 values were comparable to that of the reference cytotoxic drug cisplatin. In general, the ligands displayed only marginal inhibitory effects on the human leukemic cell lines. Moreover, the ability of the complexes to trigger apoptosis was evaluated using a commercially available DNA-fragmentation ELISA kit and the obtained data indicated that their proapoptotic effects well correlate to the MTT-bioassay data.

Key words

cytotoxicity - ruthenium(III) complexes - benzothiazole - synthesis

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