Filak Lukas K, Mühlgassner Gerhard, Bacher Felix, Roller Alexander, Galanski Markus, Jakupec Michael A, Keppler Bernhard K, Arion Vladimir B
Institute of Inorganic Chemistry, University of Vienna, Währinger Strasse 42, A-1090 Vienna, Austria.
Organometallics. 2011 Jan 24;30(2):273-283. doi: 10.1021/om101004z. Epub 2010 Dec 27.
The synthesis of new modified indolo[3,2-c]quinoline ligands L(1)-L(8) with metal-binding sites is reported. By coordination to ruthenium- and osmium-arene moieties 16 complexes of the type [(η(6)-p-cymene)M(L)Cl]Cl (1a,b-8a,b), where M is Ru(II) or Os(II) and L is L(1)-L(8), have been prepared. All compounds were comprehensively characterized by elemental analysis, electrospray ionization mass spectrometry, IR, UV-vis, and NMR spectroscopy, thermogravimetric analysis, and single-crystal X-ray diffraction (2a, 4a, 4b, 5a, 7a, and 7b). The complexes were tested for antiproliferative activity in vitro in three human cancer cell lines, namely, CH1 (ovarian carcinoma), SW480 (colon adenocarcinoma), and A549 (non-small-cell lung cancer), yielding IC(50) values in the submicromolar or low micromolar range.
报道了具有金属结合位点的新型修饰吲哚并[3,2-c]喹啉配体L(1)-L(8)的合成。通过与钌和锇芳烃部分配位，制备了[(η(6)-对异丙基苯)M(L)Cl]Cl (1a,b - 8a,b)类型的16种配合物，其中M为Ru(II)或Os(II)，L为L(1)-L(8)。所有化合物均通过元素分析、电喷雾电离质谱、红外光谱、紫外可见光谱、核磁共振光谱、热重分析和单晶X射线衍射(2a、4a、4b、5a、7a和7b)进行了全面表征。在三种人类癌细胞系，即CH1(卵巢癌)、SW480(结肠腺癌)和A549(非小细胞肺癌)中对这些配合物进行了体外抗增殖活性测试，得到的半数抑制浓度(IC(50))值在亚微摩尔或低微摩尔范围内。
