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首页> 外文期刊>RSC Advances >DNA binding, molecular docking and apoptotic inducing activity of nickel(II), copper(II) and zinc(II) complexes of pyridine-based tetrazolo[1,5-a]pyrimidine ligands
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DNA binding, molecular docking and apoptotic inducing activity of nickel(II), copper(II) and zinc(II) complexes of pyridine-based tetrazolo[1,5-a]pyrimidine ligands

机译：吡啶基四唑并[1,5-a]嘧啶配体的镍（II），铜（II）和锌（II）配合物的DNA结合，分子对接和凋亡诱导活性

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摘要

Six mononuclear copper(II), nickel(II) and zinc(II) complexes,[(MLCl2)-Cl-1] (1-3) and[M(L-2)(2)Cl-2] (4-6), of two biologically active tetrazolo[1,5-a]pyrimidine core ligands, ethyl 5-methyl-7-pyridine-2-yl-4,7-dihydrotetrazolo [1,5-a]pyrimidine-6-carboxylate (L-1) and ethyl-5-methyl-7-pyridine-4-yl-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylate (L-2), have been synthesized and characterized. The molecular structure of the ligands (L-1&2) and complex 6 were determined by single crystal X-ray diffraction. The X-ray crystal structure of 6 confirms that it has a distorted tetrahedral structure with a ZnN2Cl2 coordination environment. All of the complexes exhibit an unusually strong luminescence at room temperature. Electroparamagnetic resonance spectra of copper(II) complexes (2 and 5) show four lines, characteristic of square planar geometry, with nuclear hyperfine spin 3/2. DNA binding studies of complexes with calf-thymus DNA suggest that complexes 2 and 5 bind in the grooves of the DNA. These results were further supported by molecular docking studies. In vitro cytotoxic activities of the ligands (L-1&2) and complexes (1-6) against human cancer cell lines such as lung (A549), cervical (HeLa), colon (HCT-15) and a non-cancer human embryonic kidney cell line revealed that the complexes selectively inhibit the growth of cancer cells and are inactive against non-cancer cell lines, whereas the ligands were found to be inactive with both cancer and non-cancer cell lines. The IC50 values of the complexes revealed that the copper(II) complexes (2 and 5) exhibit high cytotoxic activity against colon (HCT-15) cells when compared to the standard drug cisplatin. Furthermore, the live cell and fluorescent imaging of cancer cells show that complexes 2 and 5 induce cell death through apoptosis.
机译：六种单核铜（II），镍（II）和锌（II）配合物，[（MLCl2）-Cl-1]（1-3）和[M（L-2）（2）Cl-2]（4- 6），两个具有生物活性的四唑并[1,5-a]嘧啶核心配体，乙基5-甲基-7-吡啶-2-基-4,7-二氢四唑并[1,5-a]嘧啶-6-羧酸盐（ L-1）和5-甲基-7-吡啶-4-基-4,7-二氢四唑[1,5-a]嘧啶-6-羧酸乙酯（L-2）已合成并表征。配体（L-1＆2）和配合物6的分子结构通过单晶X射线衍射测定。 X射线晶体结构6证实它具有扭曲的四面体结构，且具有ZnN2Cl2配位环境。所有复合物在室温下均显示出异常强的发光。铜（II）配合物（2和5）的电顺磁共振谱显示出四条线，具有正方形的平面几何形状，核自旋为3/2。复合物与小牛胸腺DNA的DNA结合研究表明，复合物2和5在DNA的凹槽中结合。这些结果得到了分子对接研究的进一步支持。配体（L-1＆2）和复合物（1-6）对人类癌细胞系（例如肺（A549），宫颈癌（HeLa），结肠（HCT-15）和非癌性人类胚胎肾）的体外细胞毒活性细胞系显示该复合物选择性地抑制癌细胞的生长，并且对非癌细胞系无活性，而发现该配体对癌细胞和非癌细胞系均无活性。配合物的IC50值表明，与标准药物顺铂相比，配合物（2和5）的铜（II）和配合物对结肠（HCT-15）细胞具有很高的细胞毒活性。此外，癌细胞的活细胞和荧光成像显示复合物2和5通过凋亡诱导细胞死亡。

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