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(Chalcogen)semicarbazones and their cobalt complexes differentiate HL-60 myeloid leukaemia cells and are cytotoxic towards tumor cell lines

机译:(硫属元素)半咔唑酮及其钴配合物可分化HL-60髓样白血病细胞并对肿瘤细胞系具有细胞毒性

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摘要

Cobalt complexes with semi- and thiosemicarbazones of 8-quinolinecarboxaldehyde have been synthesized and characterized by X-ray diffraction analysis. These novel complexes and a previously synthesized cobalt complex with a selenium-based selenosemicarbazone ligand showed myeloid differentiation activity on all trans retinoic acid resistant HL-60 acute myeloid leukaemia cells. They also showed varying levels of cytotoxicity on five human tumor cell lines: cervix carcinoma cells (HeLa), lung adenocarcinoma cells (A549), colorectal adenocarcinoma cells (LS-174), breast carcinoma cells (MDA-MB-361), and chronic myeloid leukaemia (K562) as well as one normal human cell line: fetal lung fibroblast cells (MRC-5). Leukaemia differentiation was most strongly induced by a metal-free oxygen ligand and the selenium ligand, whilst the latter and the cobalt(ii) complex with an oxygen ligand showed the strongest dose-dependent cytotoxic activity. In four out of five investigated tumor cell lines, it was of the same order of magnitude as cisplatin. These best compounds, however, had lower toxicity on non-transformed MRC-5 cells than cisplatin.
机译:合成了具有8-喹啉甲醛的半-和半-硫代咔唑的钴配合物,并通过X射线衍射分析对其进行了表征。这些新颖的复合物和先前合成的具有硒基硒代亚氨基卡巴zone配体的钴复合物对所有抗视黄酸的HL-60急性髓样白血病细胞均表现出髓样分化活性。他们还显示出对五种人类肿瘤细胞系的细胞毒性水平不同:宫颈癌细胞(HeLa),肺腺癌细胞(A549),结肠直肠腺癌细胞(LS-174),乳腺癌细胞(MDA-MB-361)和慢性骨髓白血病(K562)以及一种正常的人类细胞系:胎儿肺成纤维细胞(MRC-5)。不含金属的氧配体和硒配体最强烈地诱导了白血病的分化,而后者和具有氧配体的钴(ii)配合物表现出最强的剂量依赖性细胞毒活性。在研究的五种肿瘤细胞系中,有四种与顺铂的数量级相同。然而,这些最好的化合物对未转化的MRC-5细胞的毒性要低于顺铂。

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