title: Novel Ru(III) Complexes with Some Benzothiazole Derivatives: Synthesis, Physicochemical and Pharmacological Investigations.
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-, (1)H-NMR- (13)C-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.
authors.affiliation: Department of Chemistry, Faculty of Pharmacy, Medical University - Sofia, Sofia, Bulgaria.
authors.forename: A
authors.initials: A
authors.lastname: Nikolova
authors.affiliation: Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University - Sofia, Sofia, Bulgaria.
authors.forename: G
authors.initials: G
authors.lastname: Momekov
authors.affiliation: Department of Chemistry, Faculty of Pharmacy, Medical University - Sofia, Sofia, Bulgaria.
authors.forename: A
authors.initials: A
authors.lastname: Bakalova
authors.affiliation: Department of Chemistry, Faculty of Pharmacy, Medical University - Sofia, Sofia, Bulgaria.
authors.forename: K
authors.initials: K
authors.lastname: Nikolova
authors.affiliation: Department of Chemistry, Faculty of Pharmacy, Medical University - Sofia, Sofia, Bulgaria.
authors.forename: D
authors.initials: D
authors.lastname: Ivanov
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D052160:Benzothiazoles / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000494:pharmacology; D006801:Humans; D007938:Leukemia / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D012428:Ruthenium / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles; C005563:captax; D012428:Ruthenium; C005465:benzothiazole; D002945:Cisplatin