当前位置: X-MOL 学术RSC Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis, characterization and biological application of 5-quinoline 1,3,5-trisubstituted pyrazole based platinum(ii) complexes†
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-12-20 00:00:00 , DOI: 10.1039/c7md00472a
Miral V Lunagariya 1 , Khyati P Thakor 1 , Reena R Varma 1 , Bhargav N Waghela 2 , Chandramani Pathak 2 , Mohan N Patel 1
Affiliation  

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 K2PtCl4 salt. The synthesized compounds were characterized by micro-elemental analysis, FT-IR, UV-vis, 1H NMR, 13C NMR, TGA, mass spectrometry and molar conductivity. Their biological activities were investigated by in vitro brine shrimp lethality bioassay, in vitro antimicrobial study against five different pathogens, in vivo cellular level cytotoxicity against Schizosaccharomyces pombe cells, and in vitro anti-proliferation assay. The binding constant Ksv, Kb, Ka 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 (L1–L5) and complexes (I–V) were observed in the range of −265.14 to −284.33 kJ mol−1. The synthesized Pt(II) complexes (I–V) were screened against the MCF-7 (human breast adenocarcinoma) and HCT-116 (human colon carcinoma) cancer cell lines.

中文翻译:

5-喹啉 1,3,5-三取代吡唑基铂 (ii) 配合物的合成、表征和生物学应用†

在中性二齿杂环(5-喹啉1,3,5-三取代吡唑支架)配体和K 2 PtCl 4盐存在下合成了方形平面单核铂( II )配合物。通过微量元素分析、FT-IR、UV-vis、1 H NMR、13 C NMR、TGA、质谱和摩尔电导率对合成的化合物进行了表征。通过体外盐水虾致死率生物测定、针对五种不同病原体的体外抗菌研究、针对粟酒裂殖酵母细胞的体内细胞水平细胞毒性以及体外研究它们的生物活性。抗增殖试验。通过 DNA 相互作用研究确定了复合物的结合常数K svK bK a值。进行凝胶电泳测定以检查复合物对pUC19质粒DNA的DNA核酸酶的影响。在-265.14至-284.33 kJ mol -1范围内观察到配体( L 1 -L 5 )和配合物( I-V )的对接能。针对 MCF-7(人乳腺癌)和 HCT-116(人结肠癌)癌细胞系筛选合成的 Pt( II ) 复合物 ( I-V )。
更新日期:2017-12-20
down
wechat
bug