title: Hydrolysis and cytotoxic properties of osmium(II)/(III)-DMSO-azole complexes. Short communication.
abstract: The antiproliferative properties of the osmium(II) complexes cis,fac-[Os(II)Cl(2)(DMSO)(3)(L)] and trans,cis,cis-[Os(II)Cl(2)(DMSO)(2)(L)(2)] (L = 1H-pyrazole, 1H-imidazole) were studied in three human cancer cell lines, namely 41M (ovary), SK-BR-3 (breast), and SW480 (colon). Their activities were compared with those of osmium(III) and ruthenium(III) NAMI-A type complexes on HT-29 (colon) and SK-BR-3 cancer cell lines. While IC(50) values of all the Os(II) complexes were found to be >1000 microM in all cell lines, Os and Ru-NAMI-A type complexes showed remarkable antiproliferative activity. The marginal in vitro cytotoxicity of the Os(II) compounds is presumably attributed to their resistance to hydrolysis. However, the Os-NAMI-A complexes, which are also kinetically stable in aqueous solution, showed reasonable antiproliferative activity in vitro when compared with the analogous Ru compounds and with the Os(II)-DMSO-azole species, indicating that hydrolysis might be not a prerequisite for the antitumor activity of Os-NAMI-A type complexes.
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Alexander
authors: A
authors: Egger
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Berta
authors: B
authors: Cebrián-Losantos
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Iryna N
authors: IN
authors: Stepanenko
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Artem A
authors: AA
authors: Krokhin
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Rene
authors: R
authors: Eichinger
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Michael A
authors: MA
authors: Jakupec
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Vladimir B
authors: VB
authors: Arion
authors: University of Vienna, Institute of Inorganic Chemistry, Währingerstrasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-9526).
authors: Bernhard K
authors: BK
authors: Keppler
mesh_terms: D001393:Azoles / Q000737:chemistry / Q000633:toxicity*; D049109:Cell Proliferation / Q000187:drug effects; D004121:Dimethyl Sulfoxide / Q000737:chemistry / Q000633:toxicity*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006868:Hydrolysis / Q000187:drug effects; D008024:Ligands; D008968:Molecular Conformation; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009992:Osmium / Q000737:chemistry / Q000633:toxicity*; D012428:Ruthenium / Q000737:chemistry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D001393:Azoles; D008024:Ligands; D009942:Organometallic Compounds; D009992:Osmium; D012428:Ruthenium; D004121:Dimethyl Sulfoxide