New binuclear Cu (II) complex: synthesis, structural elucidation, cytotoxic and DNA-binding evaluation

IF 16.4 1区 化学 Q1 CHEMISTRY, MULTIDISCIPLINARY
Mouayed A. Hussein, Adyan A. Yaseen
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引用次数: 0

Abstract

A novel copper complex [Cu(μ2–OH)(1,10-phenanthroline)(4-aminobenzenesulfonic acid)·3H2O]2 (1) was synthesized and characterized by X-ray single-crystal diffraction, elemental analysis and IR spectroscopy. X-ray crystallography of complex 1 showed strictly planar bridged μ2–Cu2(OH)2 core where copper (II) center exhibited a distorted square pyramidal coordination geometry. The interaction of the complex with calf thymus DNA (CT DNA) was investigated by absorption titration and viscosity measurement. The results revealed an intercalation binding between DNA and complex 1 with a binding strength of 6.0731 × 106 ± 0.0032 M−1. The antitumor capacity of the complex was tested in vitro against human colorectal (HCT 116) cancer cell lines by metabolic tests, using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide reagent. Complex 1 showed remarkably low IC50 values of 4.844 ± 0.025 μM compared to 5-fluorouracil (7.3 μM), a widely used clinical antitumor drug.

Abstract Image

新的双核 Cu (II) 复合物:合成、结构阐明、细胞毒性和 DNA 结合评估
合成了一种新型铜配合物 [Cu(μ2-OH)(1,10-菲罗啉)(4-氨基苯磺酸)-3H2O]2(1),并通过 X 射线单晶衍射、元素分析和红外光谱对其进行了表征。复合物 1 的 X 射线晶体学显示出严格平面桥接的 μ2-Cu2(OH)2 核心,其中铜 (II) 中心呈现出扭曲的正方形金字塔配位几何。通过吸收滴定法和粘度测量法研究了该复合物与小牛胸腺 DNA(CT DNA)的相互作用。结果表明,DNA 与复合物 1 之间存在插层结合,结合强度为 6.0731 × 106 ± 0.0032 M-1。利用 3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四氮唑试剂,通过代谢测试,体外检测了复合物对人类结直肠癌(HCT 116)细胞株的抗肿瘤能力。与临床广泛使用的抗肿瘤药物 5-氟尿嘧啶(7.3 μM)相比,复合物 1 的 IC50 值明显较低,仅为 4.844 ± 0.025 μM。
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来源期刊
Accounts of Chemical Research
Accounts of Chemical Research 化学-化学综合
CiteScore
31.40
自引率
1.10%
发文量
312
审稿时长
2 months
期刊介绍: Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.
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