Anticancer activity of osmium metalla-rectangles
Anticancer activity of osmium metalla-rectangles
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DOI：
10.1039/b925015h
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发表时间：
2010-01-01
影响因子：
4
通讯作者：
Therrien, Bruno
中科院分区：
文献类型：
--
作者：
Barry, Nicolas P. E.;Edafe, Fabio;Therrien, Bruno
在甲醇中，通过与联吡啶配体[(p-伞花烃)(2)Os-2(OO布尔和OO)(2)Os-2(OO布尔和OO)(Dhbq)，2，5-二氯-1，4-苯偶氮酮(Dcbq)]反应，在甲醇中合成了一系列通式为[(p-伞花烃)(4)Os-4(OO布尔和OO)(2)(N布尔和N)(2)](4+)的阳离子金属长方形1，2-双(4-吡啶基)乙烯)。所有化合物均分离为三氟盐，并用核磁共振、红外光谱和紫外-可见光谱进行了表征。以卵巢癌细胞株A2780为实验对象，研究了双核和四核Os配合物的细胞毒作用。最具活性的金属矩形[(p-cymene)(4)Os-4(dhbq)(2)(4，4‘-bipyridine)(2)](4+)，对A2780癌细胞的IC50值为5.7µM(与顺铂相当)，对顺铂耐药的A2780cisR细胞的IC50值为7.5µM。
A series of cationic metalla-rectangles of the general formula [(p-cymene)(4)Os-4(OO boolean AND OO)(2)(N boolean AND N)(2)](4+) have been obtained in methanol from the dinuclear arene osmium precursors [(p-cymene)(2)Os-2(OO boolean AND OO)(2)Cl-2] (OO boolean AND OO = 2,5-dioxydo-1,4-benzoquinonato (dhbq), 2,5-dichloro-1,4-benzoquinonato (dcbq)) by reaction with bipyridine linkers (N boolean AND N = 4,4'-bipyridine, 1,2-bis(4-pyridyl)ethylene) in the presence of AgCF3SO3. All complexes were isolated as triflate salts and characterised by NMR, IR and UV-visible spectroscopy. The cytotoxicities of the dinuclear and tetranuclear osmium complexes were established using ovarian A2780 cancer cell lines. The most active metalla-rectangle, [(p-cymene)(4)Os-4(dhbq)(2)(4,4'-bipyridine)(2)](4+), shows an IC50 value of 5.7 mu M (comparable to cisplatin) against A2780 cancer cells and 7.5 mu M against the cisplatin resistant A2780cisR cells.