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新型水溶性 Ni(II) 配合物的合成、表征及体外药理学评价,该配合物为 2-氧代-1,2-二氢喹啉-3-甲酰基缩 4N-取代基硫代卡巴腙。

Synthesis, characterization and in vitro pharmacological evaluation of new water soluble Ni(II) complexes of 4N-substituted thiosemicarbazones of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde.

机构信息

Department of Chemistry, Bharathiar University, Coimbatore 641046, Tamil Nadu, India.

出版信息

Eur J Med Chem. 2013 Jun;64:179-89. doi: 10.1016/j.ejmech.2013.03.059. Epub 2013 Apr 6.

DOI:10.1016/j.ejmech.2013.03.059
PMID:23644201
Abstract

Four new Ni(II) complexes of general formula Ni(H2-Qtsc-R)22 (H2-Qtsc-R = 4N-substituted thiosemicarbazones of 2-oxo-1,2-dihydroquinoline-3-carbaldehyde, where R = H (1), Me (2), Et (3), or Ph (4)) have been synthesized and characterized. The geometry of the complexes was confirmed by single crystal X-ray crystallography for one of the complexes (3). The binding affinity of the complexes with DNA and protein have been studied which indicate that they could interact with calf thymus DNA and bovine serum albumin protein. Investigations of antioxidative properties showed that all the complexes have strong radical scavenging properties. Cytotoxic studies showed that the complexes exhibited effective cytotoxic activity against a panel of human cancer cells without affecting the normal cells much.

摘要

四种新的 Ni(II) 配合物的通式为Ni(H2-Qtsc-R)22(H2-Qtsc-R = 4N-取代的 2-氧代-1,2-二氢喹啉-3-甲酰腙,其中 R = H(1)、Me(2)、Et(3)或 Ph(4))已被合成并表征。其中一个配合物(3)的晶体结构通过单晶 X 射线衍射得到确认。配合物与 DNA 和蛋白质的结合亲和力研究表明,它们可以与小牛胸腺 DNA 和牛血清白蛋白蛋白相互作用。抗氧化性质的研究表明,所有配合物都具有很强的自由基清除能力。细胞毒性研究表明,这些配合物对一系列人类癌细胞具有有效的细胞毒性活性,而对正常细胞的影响很小。

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