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通过将芘基树状大分子与芳烃钌金属笼结合来增强细胞毒性。

Enhancement of cytotoxicity by combining pyrenyl-dendrimers and arene ruthenium metallacages.

机构信息

Institut de Chimie, Université de Neuchâtel, Avenue de Bellevaux 51, CH-2000 Neuchâtel, Switzerland.

出版信息

Inorg Chem. 2012 Jul 2;51(13):7119-24. doi: 10.1021/ic202739d. Epub 2012 Jun 20.

DOI:10.1021/ic202739d
PMID:22716166
Abstract

Three generations of pyrenyl bis-MPA dendrimers with two different end-groups, acetonide (pyr(Gn)) or alcohol (pyr(Gn-OH)) (n = 1-3), were synthesized, and the pyrenyl group of the dendritic molecules was encapsulated in the arene ruthenium metallacages, Ru(6)(p-cymene)(6)(OO∩OO)(3)(tpt)(2) (OO∩OO = 5,8-dioxydo-1,4-naphtaquinonato (donq) 1 and 6,11-dioxydo-5,12-naphtacenedionato (dotq) 2; tpt =2,4,6-tri(pyridin-4-yl)-1,3,5-triazine). The host-guest properties of guest⊂1 and guest⊂2 were studied in solution by NMR and UV-vis spectroscopic methods, thus allowing the determination of the affinity constants. Moreover, the cytotoxicity of these water-soluble host-guest systems and the pyrenyl-dendrimers was evaluated on human ovarian cancer cells.

摘要

三代具有两种不同端基的苯并吡喃基双-MPA 树枝状大分子,即缩酮(pyr(Gn))或醇(pyr(Gn-OH))(n = 1-3),被合成出来,树枝状分子的苯并吡喃基团被包裹在芳烃钌金属笼中,Ru(6)(p-cymene)(6)(OO∩OO)(3)(tpt)(2)(OO∩OO = 5,8-二氧代-1,4-萘醌(donq) 1 和 6,11-二氧代-5,12-萘二酮(dotq) 2;tpt = 2,4,6-三(吡啶-4-基)-1,3,5-三嗪)。通过 NMR 和紫外可见光谱法研究了guest⊂1和guest⊂2在溶液中的主体-客体性质,从而确定了亲和常数。此外,还评估了这些水溶性主客体体系和苯并吡喃基树枝状大分子对人卵巢癌细胞的细胞毒性。

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