Agents inducing apoptosis and autophagic death could be effective chemotherapeutic drugs. In this work, four novel Cu(II) complexes formulated as [CuL₂] (1), [Cu(phen)LCl]·0.5H₂O (2), [Cu₂(MQ)₂L₂] (3) and [Cu(2,2′-bpy)LCl]·H₂O (4) (phen = 1,10-Phenanthroline, HMQ = 8-hydroxy-2-methylquinoline, 2,2′-bpy = 2,2′-bipyridine) were prepared from the reactions of copper(II) chloride with tropolone (HL) in the absence or presence of different ancillary ligands. The solution state structures of 1, 2 and 4 agree well with their solid state structures. Complex 3 presents a dimer structure in the solid state, however, a monomer structure in the solution state. It was shown that all of these complexes are stable under experimental conditions and bind to DNA in an intercalative mode with the binding constant K_b values of 1.05 × 10³, 2.57 × 10³, 2.53 × 10³ and 2.26 × 10³ L mol⁻¹ for complexes 1, 2, 3 and 4, respectively. The anti-proliferative tests against cultured human cancer cell lines (A549, Bel-7402, MGC80-3, T24, SK-OV-3, and NCI-H460) in vitro revealed cytotoxic activities for these complexes, which are much better than those for all ligands in these complexes, as well as that for cis-platin. After a careful comparison, the cytotoxic activity of complex 2 against MGC80-3 cells in vitro (IC₅₀ = 3.5 ± 0.9 μM for 2 and 18.0 ± 1.2 for cis-platin) was further investigated in detail as an example. 2 induces the apoptosis of MGC80-3 through a caspase-dependent mitochondrion pathway and can also induce autophagy, which revealed a certain anticancer activity for complex 2.

中文翻译：

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带有托酚酮的四种Cu（ii）配合物的结构和抗癌活性。

诱导细胞凋亡和自噬死亡的药物可能是有效的化疗药物。在这项工作中，四种新颖的Cu（II）配合物配制成[CuL ₂ ]（1），[Cu（phen）LCl]·0.5H ₂ O（2），[Cu ₂（MQ）₂ L ₂ ]（3）和[Cu（2,2'-bpy）LCl]·H ₂ O（4）（phen = 1,10-菲咯啉，HMQ = 8-羟基-2-甲基喹啉，2,2'-bpy = 2,2' -联吡啶）是在不存在或存在不同辅助配体的情况下，由氯化铜（II）与对pol酮（HL）反应制得的。的溶液状态的结构1，2和4与其固态结构非常吻合。配合物3呈固态的二聚体结构，然而呈溶液态的单体结构。结果表明，所有这些络合物的实验条件下是稳定的并结合到DNA结合的结合常数的插入方式ķ _b的1.05×10值³，2.57×10 ³，2.53×10 ³和2.26×10 ³大号摩尔^-1用于复合物1，2，3和4， 分别。对培养人癌细胞系的抗增殖测试（A549，BEL-7402，MGC80-3，T24，SK-OV-3，和NCI-H460）在体外揭示了这些复合物的细胞毒性活性，这是要比那些更好这些复合物中的所有配体以及顺铂均适用。仔细比较，复合物的细胞毒性活性后2针对MGC80-3细胞在体外（IC ₅₀ = 3.5±0.9μM为2和18.0±1.2对顺铂）中详细描述，进一步研究，例如，2通过半胱天冬酶依赖的线粒体途径诱导MGC80-3的凋亡，并且还可以诱导自噬，从而对复合物2具有一定的抗癌活性。。