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基于5-喹啉-1,3,5-三取代吡唑的铂(II)配合物的合成、表征及生物学应用

Synthesis, characterization and biological application of 5-quinoline 1,3,5-trisubstituted pyrazole based platinum(ii) complexes.

作者信息

Lunagariya Miral V, Thakor Khyati P, Varma Reena R, Waghela Bhargav N, Pathak Chandramani, Patel Mohan N

机构信息

Department of Chemistry , Sardar Patel University , Vallabh Vidyanagar-388 120 , Gujarat , India . Email:

Department of Cell Biology , School of Biological Sciences and Biotechnology , Indian Institute of Advanced Research , Koba Institutional Area , Gandhinagar-382007 , Gujarat , India . Tel: +91 79 30514245.

出版信息

Medchemcomm. 2017 Dec 20;9(2):282-298. doi: 10.1039/c7md00472a. eCollection 2018 Feb 1.

Abstract

Square planar mononuclear platinum(ii) complexes were synthesized in the presence of neutral bidentate heterocyclic (5-quinoline 1,3,5-tri-substituted pyrazole scaffold) ligands and KPtCl salt. The synthesized compounds were characterized by micro-elemental analysis, FT-IR, UV-vis, H NMR, C NMR, TGA, mass spectrometry and molar conductivity. Their biological activities were investigated by brine shrimp lethality bioassay, antimicrobial study against five different pathogens, cellular level cytotoxicity against cells, and anti-proliferation assay. The binding constant , , values of the complexes were determined by DNA interaction studies. The gel electrophoresis assay was carried out to examine the effect of the complexes on the DNA nuclease of pUC19 plasmid DNA. The docking energies of the ligands ( ) and complexes () were observed in the range of -265.14 to -284.33 kJ mol. The synthesized Pt(ii) complexes () were screened against the MCF-7 (human breast adenocarcinoma) and HCT-116 (human colon carcinoma) cancer cell lines.

摘要

在中性双齿杂环(5-喹啉1,3,5-三取代吡唑支架)配体和氯铂酸钾盐存在的情况下合成了平面正方形单核铂(II)配合物。通过微量元素分析、傅里叶变换红外光谱、紫外可见光谱、氢核磁共振、碳核磁共振、热重分析、质谱和摩尔电导率对合成的化合物进行了表征。通过卤虫致死生物测定、针对五种不同病原体的抗菌研究、细胞水平对细胞的细胞毒性以及抗增殖测定来研究它们的生物活性。通过DNA相互作用研究确定了配合物的结合常数 、 、 值。进行凝胶电泳测定以检查配合物对pUC19质粒DNA的DNA核酸酶的影响。观察到配体( )和配合物( )的对接能量在-265.14至-284.33 kJ/mol范围内。针对MCF-7(人乳腺腺癌)和HCT-116(人结肠癌)癌细胞系筛选了合成的铂(II)配合物( )。

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