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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, structural characterization and in?vitro biological screening of some homoleptic copper(II) complexes with substituted guanidines.
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Synthesis, structural characterization and in?vitro biological screening of some homoleptic copper(II) complexes with substituted guanidines.

机译:用取代的胍对一些经络铜(II)复合物的合成,结构表征和体外生物学筛选。

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摘要

A series of homoleptic copper(II) complexes (1a-8a) with N,N',N″-trisubstituted guanidines, [Cu(II){PhCONHC(NHR)NPh}(2)] (where R?=?phenyl (1a), n-butyl (2a), sec-butyl (3a), cyclohexyl (4a), 1-naphthyl (5a), 2,4-dichlorophenyl (6a), 3,4-dichlorophenyl (7a), and 3,5-dichlorophenyl (8a)) have been synthesized and characterized by elemental analyses, FT-IR, UV-visible, (1)H and (13)C NMR spectroscopy, and single crystal X-ray diffraction analysis. The X-ray crystal structures revealed that the complexes 2a and 4a are mononuclear in the solid state and that the geometry around the copper atom is nearly square planar. In both the cases, N,N',N″-trisubstituted guanidine ligands have been coordinated to the Cu(II) through the oxygen and nitrogen atoms. The synthesized guanidines and their complexes were initially screened for their anti-microbial activities, and Brine Shrimps Lethality assay. The complexes were also screened for in?vitro cytotoxicity activity in human cell lines carcinomas A498, EVSAT, H226, IGROV, M19, MCF-7 and WIDR. The results show a moderate level of cytotoxicity against these seven human cancer cell lines as compared with standard chemotherapeutic drugs.
机译:一系列均配型铜(II)络合物(1A-8A)与N,N”,N“三取代胍,[铜(II){PhCONHC(NHR)NPH}(2)](其中,R 1 =?苯基的( 1A),正丁基(2A),仲丁基(3a)中,环己基(4A),1 - 萘基(5a)中,2,4-二氯苯基(6A),-3,4-二氯苯基(7A),和3, 5-二氯苯基(8A))已被合成和表征通过元素分析,FT-IR,UV可见,(1)H,(13)C NMR谱,和单晶X射线衍射分析。的X射线晶体结构,发现该络合物2a和图4a是在固体状态,并围绕铜原子的几何形状几乎是正方形的平面单核。在这两种情况下,N,N”,N“三取代胍配体已通过氧和氮原子配位到铜(II)。将合成的胍和它们的复合物最初筛选它们的抗微生物活性,和盐水虾致死测定。将复合物同样在人细胞系中癌A498,EVSAT,H226,IGROV,M19,MCF-7和WIDR?体外细胞毒性活性的筛选。结果表明,与标准化疗药物相比,针对这七个人类肿瘤细胞系的细胞毒性中等水平。

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