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DNA profiling and in vitro cytotoxicity studies of tetrazolo[1,5-a]pyrimidine-based copper(II) complexes.
Biometals ( IF 4.1 ) Pub Date : 2019-05-16 , DOI: 10.1007/s10534-019-00196-2
Azees Khan Haleel 1 , Ummer Muhammed Rafi 1 , Dharmasivam Mahendiran 1, 2 , Liviu Mitu 3 , Vijaykumar Veena 4 , Aziz Kalilur Rahiman 1
Affiliation  

A series of N-benzoylated mononuclear copper(II) complexes of the type [Cu(L1-6)Cl2] (1-6), where L1= ethyl 4-benzoyl-5-methyl-7-aryl-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylate, L2= ethyl 4-(4-nitrobenzoyl)-5-methyl-7-aryl-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylate, L3 = ethyl 4-benzoyl-5-methyl-7-(4-methoxyphenyl)-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylate, L4 = ethyl 4-(4-nitrobenzoyl)-5-methyl-7-(4-methoxyphenyl)-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylate, L5 = ethyl 4-benzoyl-5-methyl-7-(4-chlorophenyl)-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylate and L6 = ethyl 4-(4-nitrobenzoyl)-5-methyl-7-(4-chlorophenyl)-4,7-dihydrotetrazolo[1,5-a]pyrimidine-6-carboxylate have been synthesized and characterized by spectral methods. Electron paramagnetic resonance spectra of complexes show four lines, characteristic of square planar geometry. The binding studies of the complexes with calf thymus DNA (CT-DNA) revealed groove mode of binding, which were further supported by molecular docking studies. Gel electrophoresis experiments demonstrated the ability of the complexes to cleave plasmid DNA in the absence of activators. Further, the cytotoxicity activity of the complexes were examined on three cancerous cell lines (lung (A549), cervical (HeLa) and colon (HCT-15)), and on two normal cells (human embryonic kidney (HEK) and peripheral blood mononuclear cells (PBMC)) by MTT assay.

中文翻译:

基于四唑并[1,5-a]嘧啶的铜(II)配合物的DNA分析和体外细胞毒性研究。

一系列[Cu(L1-6)Cl2](1-6)类型的N-苯甲酰化单核铜(II)配合物,其中L1 =乙基4-苯甲酰基-5-甲基-7-芳基-4,7-二氢四唑并[1,5-a]嘧啶-6-羧酸盐,L2 = 4-(4-硝基苯甲酰基)-5-甲基-7-芳基-4,7-乙基二氢四唑并[1,5-a]嘧啶-6-羧酸盐,L3 =乙基4-苯甲酰基-5-甲基-7-(4-甲氧基苯基)-4,7-二氢四唑[1,5-a]嘧啶-6-羧酸酯,L4 =乙基4-(4-硝基苯甲酰基)-5 -甲基-7-(4-甲氧基苯基)-4,7-二氢四唑并[1,5-a]嘧啶-6-羧酸盐,L5 =乙基4-苯甲酰基-5-甲基-7-(4-氯苯基)-4, 7-二氢四唑[1,5-a]嘧啶-6-羧酸盐,L6 = 4-(4-硝基苯甲酰基)-5-甲基-7-(4-氯苯基)-4,7-二氢四唑[1,5-a]已经合成了嘧啶-6-羧酸盐并通过光谱方法表征。配合物的电子顺磁共振谱显示出四条线,方形平面几何的特征。配合物与小牛胸腺DNA(CT-DNA)的结合研究揭示了沟的结合模式,这进一步得到分子对接研究的支持。凝胶电泳实验证明了在没有激活剂的情况下复合物切割质粒DNA的能力。此外,在三种癌细胞系(肺癌(A549),宫颈癌(HeLa)和结肠癌(HCT-15))以及两种正常细胞(人胚肾(HEK)和外周血单核细胞)上检查了复合物的细胞毒性活性。细胞(PBMC))。凝胶电泳实验证明了在没有激活剂的情况下复合物切割质粒DNA的能力。此外,在三种癌细胞系(肺癌(A549),宫颈癌(HeLa)和结肠癌(HCT-15))以及两种正常细胞(人胚肾(HEK)和外周血单核细胞)上检查了复合物的细胞毒性活性。细胞(PBMC))。凝胶电泳实验证明了在没有激活剂的情况下复合物切割质粒DNA的能力。此外,在三种癌细胞系(肺癌(A549),宫颈癌(HeLa)和结肠癌(HCT-15))以及两种正常细胞(人胚肾(HEK)和外周血单核细胞)上检查了复合物的细胞毒性活性。细胞(PBMC))。
更新日期:2019-11-01
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