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Organometallic nucleoside analogues: effect of the metallocene metal atom on cancer cell line toxicity†
Dalton Transactions ( IF 4 ) Pub Date : 2019-12-16 , DOI: 10.1039/c9dt04174e
Media K. Ismail 1, 2, 3, 4 , Katie A. Armstrong 2, 3, 4, 5 , Samantha L. Hodder 2, 3, 4, 5 , Sarah L. Horswell 1, 2, 3, 4 , Louise Male 1, 2, 3, 4 , Huy V. Nguyen 1, 2, 3, 4 , Edward A. Wilkinson 1, 2, 3, 4 , Nikolas J. Hodges 2, 3, 4, 5 , James H. R. Tucker 1, 2, 3, 4
Affiliation  

A new chiral organometallic nucleoside analogue containing ruthenocene is reported, in which alkylthymine and alkylhydroxyl groups are attached in adjacent positions on one cyclopentadienyl ring. The synthetic procedures for this metallocene derivative and two control compounds are described, along with their characterisation by cyclic voltammetry and X-ray crystallography. Their biological activities in a human pancreatic cancer cell line (MIA-Pa-Ca-2) were significantly lower than those of three previously reported analogous ferrocene compounds, indicating that the choice of metallocene metal atom (Fe or Ru) plays a pivotal role in determining the anticancer properties of these nucleoside analogues, which in turn suggests a different mode of action from that of a conventional nucleoside analogue.

中文翻译:

有机金属核苷类似物:茂金属原子对癌细胞系毒性的影响

报道了一种新的含有钌茂茂的手性有机金属核苷类似物,其中烷基胸腺嘧啶和烷基羟基连接在一个环戊二烯基环的相邻位置。描述了该茂金属衍生物和两种对照化合物的合成方法,以及通过循环伏安法和X射线晶体学对其进行表征的方法。它们在人胰腺癌细胞系(MIA-Pa-Ca-2)中的生物学活性显着低于先前报道的三种类似的二茂铁化合物,这表明金属茂金属原子(Fe或Ru)的选择起着至关重要的作用。确定这些核苷类似物的抗癌特性,这反过来表明与常规核苷类似物具有不同的作用方式。
更新日期:2020-01-04
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