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含亲脂性侧链的半三明治型铑和铱金属棱柱体的抗癌活性

Anticancer Activity of Half-Sandwich Rh and Ir Metalla-Prisms Containing Lipophilic Side Chains.

作者信息

Gupta Gajendra, Mahesh Kumar Jerald, Garci Amine, Rangaraj Nandini, Nagesh Narayana, Therrien Bruno

机构信息

Institute of Chemistry, University of Neuchatel, Ave. de Bellevaux 51, 2000 Neuchatel (Switzerland).

CSIR-Centre for Cellular and Molecular Biology, Uppal Road, Habsiguda, Hyderabad 500 007 (India).

出版信息

Chempluschem. 2014 Apr;79(4):610-618. doi: 10.1002/cplu.201300425. Epub 2014 Mar 11.

Abstract

Two hexacationic pentamethylcyclopentadienyl rhodium(III) and iridium(III) metalla-prisms, [(η -C Me ) M (μ -tpt-κN) (μ -C HRO -κO) ] (tpt=2,4,6-tri-(pyridin-4-yl)-1,3,5-triazine; R=(CH ) CH ; M=Rh, [3] ; M=Ir, [4] ) isolated as their triflate salts, have been synthesised from the dinuclear complexes (η -C Me ) M (μ -C HRO -κO)Cl (M=Rh, 1; M=Ir, 2) and AgCF SO . The antiproliferative activity of the neutral and cationic complexes has been evaluated in vitro in human cancer cell lines. The positively charged metalla-prisms appear to target mitochondria, which ultimately induce apoptosis in cancer cells. All biological studies suggest that the rhodium derivative [3][CF SO ] possesses excellent activities, not only in vitro but also in vivo in tumour-induced C57L6/J mice.

摘要

两种六阳离子五甲基环戊二烯基铑(III)和铱(III)金属棱柱,即[(η⁵-C₅Me₅)₂M(μ₃-tpt-κ³N)(μ₂-C₆H₄RO₂-κ²O)](tpt = 2,4,6-三(吡啶-4-基)-1,3,5-三嗪;R = (CH₂)₃CH₃;M = Rh,[3];M = Ir,[4])以其三氟甲磺酸盐形式分离得到,是由双核配合物(η⁵-C₅Me₅)₂M(μ₂-C₆H₄RO₂-κ²O)Cl(M = Rh,1;M = Ir,2)和AgCF₃SO₃合成的。中性和阳离子配合物的抗增殖活性已在体外人癌细胞系中进行了评估。带正电荷的金属棱柱似乎靶向线粒体,最终诱导癌细胞凋亡。所有生物学研究表明,铑衍生物[3][CF₃SO₃]不仅在体外而且在肿瘤诱导的C57L6/J小鼠体内均具有优异的活性。

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