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Anticancer activity of self-assembled molecular rectangles via arene-ruthenium acceptors and a new unsymmetrical amide ligand

机译:通过芳烃-钌受体和新的不对称酰胺配体自组装分子矩形的抗癌活性

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摘要

Two new and large molecular rectangles 4 and 5 were synthesized from two different arene-ruthenium [Ru _2(μ-η ~4-C _2O _4)(MeOH) _2(η ~6-p-Pr ~iC _6H _4Me) _2][O _3SCF _3] _2 (2) and [Ru _2(p-cymene) _2(donq) (OH _2) _2][O _3SCF _3] _2 (donq = 5,8-dioxydo-1,4-naphthaquinonato) (3) acceptors and a new unsymmetrical N-(4-(pyridin-4-ylethynyl)phenyl) isonicotinamide (1) donor ligand. X-ray crystallography of 4 confirmed a molecular rectangle. The 1H NMR spectra of both rectangles 4 and 5 showed a mixture of two structural, head-to-tail (HTT) and head-to-head (HTH), type isomers in a 1:1 ratio. The cytotoxicities of both rectangles have been established against Colo320 (colorectal cancer), A549 (lung cancer), MCF-7 (breast cancer), and H1299 (lung cancer) human cancer cell lines. The cytotoxicity of rectangle 5 was found to be considerably stronger against all cancer cell lines than that of the reference drug cisplatin.
机译:由两个不同的芳烃钌[Ru _2(μ-η〜4-C _2O _4)(MeOH)_2(η〜6-p-Pr〜iC _6H _4Me)_2合成了两个新的大分子矩形4和5。 [O _3SCF _3] _2(2)和[Ru _2(对苯甲基)_2(donq)(OH _2)_2] [O _3SCF _3] _2(donq = 5,8-dioxydo-1,4-naphthaquinonato)( 3)受体和新的不对称N-(4-(吡啶-4-基乙炔基)苯基)异烟酰胺(1)供体配体。 4的X射线晶体学证实为分子矩形。两个矩形4和5的1H NMR谱图显示了两种结构的头对尾(HTT)和头对头(HTH)型异构体的比例为1:1的混合物。已经建立了两个矩形对Colo320(结肠直肠癌),A549(肺癌),MCF-7(乳腺癌)和H1299(肺癌)人癌细胞系的细胞毒性。发现矩形5对所有癌细胞的细胞毒性比参考药物顺铂强。

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