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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Cytotoxic activity of new neodymium (III) complexes of bis-coumarins.
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Cytotoxic activity of new neodymium (III) complexes of bis-coumarins.

机译：双香豆素新钕（III）配合物的细胞毒活性。

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摘要

Complexes of neodymium (III) with bis-coumarins: 3,3'-benzylidene-bis(4-hydroxy-2H-1-benzopyran-2-one); bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-piridin-2-yl-methane; bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-piridin-4-yl-methane; bis(4-hydroxy-2-oxo-2H-chromen-3-yl)-(1H-pyrazol-3-yl)-methane were synthesized by reaction of neodymium (III) salt and the ligands, in amounts equal to metal:ligand molar ratio of 1:2. The complexes were prepared by adding an aqueous solution of neodymium (III) salt to an aqueous solution of the ligand subsequently raising the pH of the mixture gradually to ca. 5.0 by adding dilute solution of sodium hydroxide. The neodymium (III) complexes with bis-coumarins were characterized by different physicochemical methods-elemental analysis, IR-, (1)H- and (13)C-NMR-spectroscopies and mass-spectral data. The spectral data of neodymium (III) complexes were interpreted on the basis of comparison with the spectra of the free ligands. This analysis showed that in the Nd (III) complexes the ligands coordinated to the metal ion through both deprotonated hydroxyl groups. On the basis of the nu(C=O) red shift observed, participation of the carbonyl groups in the coordination to the metal ion was also suggested. Cytotoxic screening by MTT assay was carried out. The complexes were tested on HL-60, HL-60/Dox and SKW-3 cell lines. The overall results from the preliminary screening program revealed that all of the new Nd (III) complexes reach 50% inhibition of the malignant cells proliferation and thus could be considered as biologically active. On the basis of the IC(50) values obtained compounds Nd(L(1))(OH).H(2)O and Nd(L(3))(OH).2H(2)O were found to exert superior activity in comparison to the remaining complexes.
机译：钕（III）与双香豆素的配合物：3,3'-亚苄基-双（4-羟基-2H-1-苯并吡喃-2-酮）;双（4-羟基-2-氧代-2H-铬-3-基）-吡啶-2-基-甲烷;双（4-羟基-2-氧代-2H-铬-3-基）-吡啶-4-基-甲烷;通过钕（III）盐与配体的反应合成双（4-羟基-2-氧代-2H-铬-3-基）-（1H-吡唑-3-基）-甲烷，其数量等于金属：配体摩尔比为1：2。通过将钕（III）盐的水溶液添加到配体的水溶液中，然后将混合物的pH逐渐升高至约3，1，3，3，3，4，4，5-二氧杂苯并呋喃，制备配合物。 5.0加入氢氧化钠稀溶液。具有双香豆素的钕（III）配合物通过不同的理化方法-元素分析，IR-，（1）H-和（13）C-NMR光谱和质谱数据进行了表征。在与游离配体的光谱比较的基础上解释了钕（III）配合物的光谱数据。该分析表明，在Nd（III）配合物中，配体通过两个去质子化的羟基与金属离子配位。基于观察到的nu（C ＝ O）红移，还建议羰基参与金属离子的配位。通过MTT测定进行细胞毒性筛选。在HL-60，HL-60 / Dox和SKW-3细胞系上测试了复合物。初步筛选程序的总体结果显示，所有新的Nd（III）复合物均达到50％抑制恶性细胞增殖的作用，因此可以认为具有生物活性。根据IC（50）值，发现化合物Nd（L（1））（OH）.H（2）O和Nd（L（3））（OH）.2H（2）O表现出优异的性能。与其余复合物相比的活性。

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