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Electronic effects on reactivity and anticancer activity by half-sandwich N,N-chelated iridium(iii) complexes†
New Journal of Chemistry ( IF 3.3 ) Pub Date : 2018-09-04 00:00:00 , DOI: 10.1039/c8nj03360a
Lihua Guo 1, 2, 3 , Hairong Zhang 1, 2, 3 , Meng Tian 1, 2, 3 , Zhenzhen Tian 1, 2, 3 , Yanjian Xu 1, 2, 3 , Yuliang Yang 1, 2, 3 , Hongwei Peng 1, 2, 3 , Peng Liu 1, 2, 3 , Zhe Liu 1, 2, 3
Affiliation  

The synthesis and characterization of a series of organometallic half-sandwich N,N-chelated iridium(III) complexes bearing a range of electron-donating and withdrawing substituents were described. The X-ray crystal structures of complexes 1, 3 and 5 have been determined. This work demonstrated how the aqueous chemistry, catalytic activity in converting coenzyme NADH to NAD+ and anticancer activity can be controlled and fine-tuned by the modification of the ligand electronic perturbations. In general, the introduction of an electron-withdrawing group (–Cl and –NO2) on the bipyridine ring resulted in increased anticancer activity, whereas an electron-donating group (–NH2, –OH and –OCH3) decreased the anticancer activity. Complex 6 bearing a strongly electron-withdrawing NO2 group displayed the highest anticancer activity (7.3 ± 1.2 μM), ca. three times as active as cisplatin in the A549 cell line. Notably, selective cytotoxicity for cancer cells over normal cells was observed for complexes 1 and 6. DNA binding does not seem to be the primary mechanism for cancer fighting. However, the aqueous chemistry, cell apoptosis and cell cycle, which show similar dependence on the ligand electronic perturbations as the anticancer activity, appear to together contribute to the anticancer potency of theses complexes. This work may provide an alternative strategy to enhance anticancer activity for these N,N-chelated organometallic half-sandwich iridium(III) complexes.

中文翻译:

半三明治N,N螯合铱(iii)配合物对反应性和抗癌活性的电子影响

描述了一系列带有一系列给电子和吸电子取代基的有机金属半三明治N,N螯合铱(III)配合物的合成和表征。复合物的X射线晶体结构135已经被确定。这项工作证明了如何通过修饰配体电子扰动来控制和微调水溶液的化学性质,将辅酶NADH转化为NAD +的催化活性和抗癌活性。通常,在联吡啶环上引入吸电子基团(–Cl和–NO 2)会提高抗癌活性,而给电子基团(–NH 2,-OH和-OCH 3)降低了抗癌活性。带有强吸电子NO 2基团的配合物6表现出最高的抗癌活性(7.3±1.2μM),约为。在A549细胞系中的活性是顺铂的三倍。值得注意的是,复合物16观察到对癌细胞的选择性细胞毒性超过正常细胞。DNA结合似乎不是抗癌的主要机制。然而,水化学,细胞凋亡和细胞周期显示出与抗癌活性类似的对配体电子干扰的依赖性,似乎共同促进了这些复合物的抗癌效力。这项工作可能为增强这些N,N螯合的有机金属半夹心铱(III)配合物的抗癌活性提供替代策略。
更新日期:2018-09-04
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