title: Ruthenium- and osmium-arene complexes of 8-substituted indolo[3,2-c]quinolines: Synthesis, X-ray diffraction structures, spectroscopic properties, and antiproliferative activity.
abstract: Six novel ruthenium(II)- and osmium(II)-arene complexes with indoloquinoline modified ligands containing methyl and halo substituents in position 8 of the molecule backbone have been synthesised and comprehensively characterised by spectroscopic methods (1H,13C NMR, UV-Vis), ESI mass spectrometry and X-ray crystallography. Binding of indoloquinolines to a metal-arene scaffold makes the products soluble enough in biological media to allow for assaying their antiproliferative activity. The complexes were tested in three human cancer cell lines, namely A549 (non-small cell lung cancer), SW480 (colon carcinoma) and CH1 (ovarian carcinoma), yielding IC50values in the 10-6-10-7M concentration range after continuous exposure for 96 h. Compounds with halo substituents in position 8 are more effective cytotoxic agentsin vitrothan the previously reported species halogenated in position 2 of the indoloquinoline backbone. High antiproliferative activity of both series of substances may be due at least in part to their potential to act as DNA intercalators.
authors.affiliation: Institute of Inorganic Chemistry, University of Vienna, Währinger Strasse 42, 1090 Vienna, Austria.
authors.forename: Lukas K
authors.initials: LK
authors.lastname: Filak
authors.forename: Simone
authors.initials: S
authors.lastname: Göschl
authors.forename: Stefanie
authors.initials: S
authors.lastname: Hackl
authors.forename: Michael A
authors.initials: MA
authors.lastname: Jakupec
authors.forename: Vladimir B
authors.initials: VB
authors.lastname: Arion
keywords: Anticancer compound; Indolo[3,2-c]quinoline; Osmium(II); Ruthenium(II)