Highly active neutral ruthenium(II) arene complexes: Synthesis, characterization, and investigation of their anticancer properties

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• 作者：Gerd Ludwig ; Goran N. Kalu?erovi? ; Martin Bette ; Michael Block ; Reinhard Paschke ; Dirk Steinborn
• 关键词：Ruthenium(II) complexes ; P ; S ligands ; Cytotoxic activity
• 刊名：Journal of Inorganic Biochemistry
• 出版年：2012
• 出版时间：August, 2012
• 年：2012
• 卷：113
• 期：Complete
• 页码：77-82
• 全文大小：830 K

文摘

Reactions of ¦Ø-diphenylphosphino-functionalized alkyl phenyl sulfides Ph₂P(CH₂)_nSPh (n = 1, L1; 2, L2; 3, L3), sulfoxides Ph₂P(CH₂)_nS(O)Ph (n = 1, L4; 2, L5; 3, L6) and sulfones Ph₂P(CH₂)_nS(O)₂Ph (n = 1, L7; 2, L8; 3, L9) with the dinuclear chlorido bridged ruthenium(II) complex [{Ru(¦Ç⁶-p-cymene)Cl₂}₂] afforded mononuclear ruthenium(II) complexes of the type [Ru(¦Ç⁶-p-cymene)Cl₂{Ph₂P(CH₂)_nS(O)_xPh-¦ÊP}] (n/x = 1/0, 1; 2/0, 2; 3/0, 3; 1/1, 4; 2/1, 5; 3/1, 6; 1/2, 7; 2/2, 8; 3/2, 9) having the P^¡ÉS(O)_x ligands ¦ÊP coordinated. The complexes were characterized by ¹H, ¹³C and ³¹P NMR spectroscopy. The crystal structures of complexes 2, 7¡¤CH₂Cl₂ and 8 were determined by X-ray diffraction analysis. All complexes have been screened for cytostatic activity against cell lines 518A2, 8505C, A253, MCF-7, and SW480. In vitro biological experiments demonstrate that these compounds are active toward the used cell lines. The ruthenium(II) complex [Ru(¦Ç⁶-p-cymene)Cl₂{Ph₂P(CH₂)₂SPh-¦ÊP}] (2) is the most active compound in the human cancer cell line MCF-7 with the IC₅₀ value 1.4 ¦ÌM lower than cisplatin (2.0 ¦ÌM).