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双吗啉取代吡啶锌和铜配合物的合成、表征及抗癌活性初步研究

汪清清 潘耀 游双 黄鑫 熊衍才 王小波

湖北科技学院学报(医学版)2024,Vol.38Issue(4):292-296,5.
湖北科技学院学报(医学版)2024,Vol.38Issue(4):292-296,5.DOI:10.16751/j.cnki.2095-4646.2024.04.0292

双吗啉取代吡啶锌和铜配合物的合成、表征及抗癌活性初步研究

Preliminary Studies of Synthesis,Characterization and Anticancer Activity of Zinc and Copper Complexes Based on Bis-Morpholine Substituted Pyridine

汪清清 1潘耀 1游双 1黄鑫 1熊衍才 1王小波1

作者信息

  • 1. 湖北科技学院医学部药学院,湖北 咸宁 437100
  • 折叠

摘要

Abstract

Objective To research the synthesis and anticancer activities of zinc and copper complexes based on bis-mor-pholine substituted pyridine(Mor2-Py-Zn and Mor2-Py-Cu).Methods Taking the antagonist AMD3100,which entered the clinical trial,as the lead compound,Mor2-Py-Zn and Mor2-Py-Cu were designed and synthesized,and characterized by high resolution mass spectrometry.The crystal structure was determined by X-ray single crystal diffraction.The interaction between complexes and calf thymus DNA(CT-DNA)was studied by UV-Vis absorption spectroscopy,and the cytotoxicity against glioblastoma cells was further studied by morphological analysis and MTT assays.Results Mor2-Py-Zn belongs to the orthorhombic system,pbca space group,pyr-idine N,two morpholine N and two nitrate O atoms form a triangular bipyramidal configuration of N3O2 pentagram with Zn2+.Both Mor2-Py-Zn and Mor2-Py-Cu interacted with CT-DNA in solution to some extent.The two complexes showed weak inhibitory activi-ty against U87,but obviously inhibited the proliferation of U251.Further,MTT assay showed that the IC50 of Mor2-Py-Zn and Mor2-Py-Cu for U251 cells were 18.11μmol/L and 14.66 μmol/L,respectively.Conclusion Both Mor2-Py-Zn and Mor2-Py-Cu are val-uable for further study of their anticancer mechanism,especially for U251 cells.

关键词

锌配合物/铜配合物/抗癌/人胶质瘤细胞/DNA相互作用/晶体结构

Key words

Zinc complex/Copper complex/Anticancer/Glioma cells/Interaction with DNA/Crystal structure

分类

医药卫生

引用本文复制引用

汪清清,潘耀,游双,黄鑫,熊衍才,王小波..双吗啉取代吡啶锌和铜配合物的合成、表征及抗癌活性初步研究[J].湖北科技学院学报(医学版),2024,38(4):292-296,5.

基金项目

湖北省教育厅重点项目(D20212802) (D20212802)

湖北科技学院学报(医学版)

2095-4646

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