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Luminescent iminophosphorane gold palladium and platinum complexes as potential anticancer agents

机译:发光亚氨基磷烷金钯和铂配合物可能用作抗癌剂

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摘要

A series of coordination gold(III), palladium(II), and platinum(II) complexes with a luminescent iminophosphorane ligand derived from 8-aminoquinoline [Ph3P=N-C9H6N] (>1), have been synthesized and structurally characterized. The coordination palladium(II) and platinum(II) compounds can evolve further, under appropriate conditions, to give stable cyclometalated endo species [M{κ3-C,N,N-C6H4(PPh2=N-8-C9H6N}Cl] (M = Pd, Pt) by C-H activation of the phenyl group of the PPh 3 fragment. Iminophosphorane >1 and the new metallic complexes are luminescent in DMSO or DMSO:H2O (1:1 mixture) solutions at RT. The compounds have been evaluated for their antiproliferative properties in a human ovarian cancer cell line (A2780S), in human lung cancer cells (A-549) and in a non-tumorigenic human embryonic kidney cell line (HEK-293T). Most compounds have been more toxic to the ovarian cancer cell line than to the non-tumorigenic cell line. The new complexes interact with human serum albumin (HSA) faster than cisplatin. Studies of the interactions of the compounds with DNA indicate that, in some cases, they exert anticancer effects in vitro based on different mechanisms of action with respect to cisplatin.
机译:一系列具有8-氨基喹啉[Ph3P = N-C9H6N](> 1 )的发光亚氨基磷烷配体的配位金(III),钯(II)和铂(II)配合物合成并进行结构表征。在适当的条件下,配位的钯(II)和铂(II)化合物可以进一步演化,从而生成稳定的环金属化内生物种[M {κ 3 -C,N,N-C6H4(PPh2 = N -8-C9H6N} Cl](M = Pd,Pt),通过CH活化PPh 3片段的苯基。亚氨基磷烷> 1 和新的金属配合物在DMSO或DMSO:H2O中发光(在室温下以1:1的比例)溶液对化合物进行了评估,这些化合物在人卵巢癌细胞系(A2780S),人肺癌细胞(A-549)和非致瘤性人胚胎肾细胞系中具有抗增殖作用(HEK-293T)。大多数化合物对卵巢癌细胞系的毒性要大于对非肿瘤细胞系的毒性。新复合物与人血清白蛋白(HSA)的相互作用要快于顺铂。 DNA表明,在某些情况下,它们基于顺式作用的不同作用机制在体外发挥抗癌作用铂金。

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