ARTICLE DOI: 10.1002/zaac.201300054 Osmium-Nitrosyl Complexes with Glycine, Picolinic Acid, L-Proline and D-Proline: Synthesis, Structures and Antiproliferative Activity Anatolie Gavriluta, [a] Maria Novak, [b] Jean Bernard Tommasino, [a] Samuel M. Meier, [b] Michael A. Jakupec, [b] Dominique Luneau,* [a] and Vladimir B. Arion* [b] Keywords: Osmium; Amino acids; Bioinorganic chemistry; Cytotoxicity Abstract. The reactions of [Os(NO)Cl 5 ] 2– with glycine (GlyH), pico- linic acid (PicoH), -proline (-ProH) and -proline (-ProH) afforded four novel complexes of the general formula [Os(NO)Cl 3 (AA)] , where AA = Gly, Pico, -Pro and -Pro, respectively. X-ray diffraction studies have revealed that in all cases the same isomer type from three Introduction The antitumor activity of metal based drugs depends upon many parameters, [1] including the reactivity towards amino ac- ids, the most important low-molecular-weight biological li- gands. Investigation of these reactions can help in establish- ment of the nature of the species delivered into the cells, since the compounds can be modified inside the human body, in getting insight into the mechanisms of detoxification and me- tabolism of applied drugs, and in identification of potential cellular targets responsible for cytotoxicity. [2] For instance, a platinum(II) compound with -methionine, Pt(L-met) 2 , was isolated from human urine, while studying the metabolism of cisplatin in the human body. [3] The effect of cell culture media, consisting mainly of amino acids, salts (Na + ,K + , Mg 2+ , Ca 2+ ), vitamins and glucose, on the metal-based drugs is a standard test now to probe their resistance to a chemical environment on application in vitro in cell culture experiments. Quite recently, we prepared a series of ruthenium(II)- and osmium(II)-nitrosyl complexes with azole ligands and found out that they show a striking difference in antiproliferative ac- tivity, in strong contrast to previous comparative studies of homologous ruthenium(II) and osmium(II) complexes. [4] Within a more extended program initiated recently, we are try- * Prof. Dr. D. Luneau E-Mail: dominique.luneau@univ-lyon1.fr * Prof. Dr. V. Arion E-Mail: vladimir.arion@univie.ac.at [a] Université Claude Bernard Lyon 1 Laboratoire des Multimatériaux et Interfaces (UMR 5615) Campus de La Doua 69622 Villeurbanne Cedex, France [b] University of Vienna Institute of Inorganic Chemistry Währinger Strasse 42 1090 Vienna, Austria Supporting information for this article is available on the WWW under http://dx.doi.org/10.1002/zaac.201300054 or from the au- thor. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim Z. Anorg. Allg. Chem. 2013, 639, (8-9), 1590–1597 1590 theoretically possible, has been isolated, namely mer(Cl), trans(NO,O)-[Os(NO)Cl 3 (AA)] . Spectroscopic and electrochemical properties, behavior in aqueous solution and antiproliferative activity in three human cancer cell lines are also reported. ing to find out the reasons for the observed difference in cyto- toxicity. Nitric oxide plays important roles in biochemical pro- cesses. [5] It is a typical example of a non-innocent ligand [6] in coordination chemistry. It binds to metals linearly (NO + ) or adopting a bent mode (NO ). The linearly coordinated NO + ligand is a poor σ-donor, but a very strong π-acceptor. NO + shows a range of structural trans effects (STEs) depending upon the identity of the trans ligand. [7] Generally trans M–L bonds to π-acceptor ligands (NO, CO) are lengthened due to competition for π-electron density, while π-donation from chlorido or hydroxido ligands, stimulated by the strong π-ac- ceptor nature of NO + , results in inverse STEs, namely, shorten- ing of both trans bonds M–NO + and M–L trans . In addition, the metal-nitrosyl unit acts as a reaction mediator or regulator of geometry around the metal atom. [8] Linkage isomerization of the N- and O-bonded nitrosyl ligands is also well-documen- ted. [9] Despite great interest of researchers in this type of com- pounds, very little is known about the reactivity of rutheni- um(II)-nitrosyl compounds with amino acids, [9b,10] while data on the related osmium counterparts to the best of our knowl- edge have not been reported so far. The only well-characterized osmium compounds with amino acids are osmyl(VI) complexes with glycine, DL-alanine, DL- valine, DL-leucine, DL-isoleucine, DL-phenylalanine ligands reported more than 30 years ago, [11] and osmium(II)-arene compounds with -prolinate, namely, [(η 6 -p-cymene)Os(L- prolinate)] 3 [BF 4 ] 3 , [12] and [OsCl(CO)(L-phenylalaninate)- (PPh 3 ) 2 ]. [13] All this prompted us to initiate the study of the reactions of [Os(NO)Cl 5 ] 2– with some potentially bidentate amino acids in order to elucidate the effect of coordinated NO + on the nature of the favored co-ligand in trans-position and on the favored isomer type formed, to isolate and fully characterize the reac- tion products and evaluate their antiproliferative activity in hu- man cancer cell lines. Herein we report on the synthesis of four