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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >New gold pincer-type complexes: synthesis, characterization, DNA binding studies and cytotoxicity
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New gold pincer-type complexes: synthesis, characterization, DNA binding studies and cytotoxicity

机译：新的金钳式复合物：合成，表征，DNA结合研究和细胞毒性

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With the aim of assessing whether Au(iii) compounds with pincer type ligands might be utilized as potential antitumor agents, three new monofunctional Au(iii) complexes of the general formula [Au(N-N'-N)Cl]Cl-2, where N-N'-N = 2,6-bis(5-tert-butyl-1H-pyrazol-3-yl)pyridine (H2LtBu, 1), 2,6-bis(5-tert-butyl-1-methyl-1H-pyrazol-3-yl)pyridine (Me2LtBu, 2) or 2,6-bis((4S,7R)-1,7,8,8-tetramethyl-4,5,6,7-tetrahydro-1H-4,7-methanoindazol-3-yl)pyridine (Me-2*L, 3) were synthesized. All complexes were characterized by elemental analysis, spectroscopic techniques (IR, UV-Vis, 1D and 2D NMR) and mass spectrometry (MALDI TOF MS). The chemical behavior of the complexes under physiological conditions was studied by UV-Vis spectroscopy, which showed that all compounds were remarkably stable and that the gold center remained in the 3+ oxidation state. The kinetics and the mechanism of the reaction of complexes 1-3 with guanine derivatives (i.e. guanosine (Guo) and guanosine-5-monophosphate (5-GMP)) and calf thymus DNA (CT DNA) were studied by stopped-flow spectroscopy. The three complexes displayed moderately different rate constants in their reactions with Guo, 5-GMP and CT DNA, which can be explained by the steric hindrance and sigma-donicity of the methyl substituent on the bis-pyrazolylpyridine fragment in complexes 2 and 3. The measured enthalpies and entropies of activation (Delta H-not equal 0, Delta S-not equal 0) supported an associative mechanism for the substitution process. The interaction of the newly synthesized complexes 1-3 with CT DNA was investigated by UV-Vis and fluorescence spectroscopy, and also by viscosity measurements, which all indicated that complexes 1-3 bound to CT DNA with moderate binding affinity (K-b = 1.6-5.7 x 10(3) M-1) and stabilized the duplex of CT DNA. Molecular docking indicated that complexes 1-3 interacted with DNA via intercalation. Complex 1 reduced the cell survival of all the investigated cell lines (A549, A375, and LS-174) wi
机译：目的是评估与钳式配体的Au（III）化合物是否可用作潜在的抗肿瘤剂，通式[Au（N-N'-N）Cl] Cl-2的三种新的单官能Au（III）复合物。 ，其中N-N'-N = 2,6-双（5-叔丁基-1H-吡唑-3-基）吡啶（H2LTBU，1），2,6-双（5-叔丁基-1-甲基-1H-吡唑-3-基）吡啶（ME2LTBU，2）或2,6-双（（4S，7R）-1,7,8,8-四甲基-4,5,6,7-四氢-1H合成-4,7-甲基吲哚-3-基）吡啶（ME-2 * L，3）。通过元素分析，光谱技术（IR，UV-Vis，1D和2D NMR）和质谱（MALDI TOF MS），所有复合物的特征在于。通过UV-Vis光谱研究了生理条件下复合物的化学行为，表明所有化合物都非常稳定，并且金中心仍然是3+氧化​​态。通过停止流动光谱研究了与鸟嘌呤衍生物的络合物1-3与络合物1-3反应的络合物1-3反应的机理（即鸟苷（GUO）和鸟苷-5-单磷酸（5-GMP））和小牛胸腺DNA（CT DNA）。三种复合物在其与GUO，5-GMP和CT DNA的反应中显示的三种复合物，其可以通过络合物2和3中的双吡唑基吡啶片段上的空间障碍和甲基取代基的空间障碍和Sigma奖励来解释测量的激活焓和熵（Delta H-not等于＆ 0，ΔS-not等于＆ 0）支持替代过程的关联机制。通过UV-Vis和荧光光谱研究新合成的复合物1-3与CT DNA的相互作用，以及粘度测量，所有这些都表明复合物1-3与CT DNA结合，中等结合亲和力（KB = 1.6- 5.7 x 10（3）m-1）并稳定CT DNA的双链体。分子对接表明复合物1-3通过插层与DNA相互作用。复合体1减少了所有研究的细胞系（A549，A375和LS-174）的细胞存活率

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