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Evolution of 1, 3, 5-trisubstituted bipyrazole scaffold based platinum(ll) complexes as a biological active agent

机译:作为生物活性剂的1,3,5-三取代的双吡唑支架基铂(LL)复合物的演化

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摘要

Square planar mononuclear platinum(ll) complexes having general formula [Pt(Ln)CI2], (where, Ln = L^4) were synthesized with neutral bidentate heterocyclic 1,3,5-trisubstituted bipyrazole based ligands. The synthesized compounds were characterized by physicochemical method such as TGA, molar conductance, micro-elemental analysis and magnetic moment, and spectro-scopic method such as, FT-IR, UV-vis, nH NMR, 13C NMR and mass spectrometry. Biological applications of the compounds were carried out using in vitro brine shrimp lethality bioassay, in vitro antimicrobial study against five different pathogens, and cellular level cytotoxicity against Schizosaccharomyces pombe (5. Pombe) cells. Pt(ll) complexes were tested for DNA interaction activities using electronic absorption titration, viscosity measurements study, fluorescence quenching technique and molecular docking assay. Binding constants {Kb) of ligands and complexes were observed in the range of 0.23-1.07 x 105M^n and 0.51-3.13 x 105M^ respectively. Pt(ll) complexes (IIV) display an excellent binding tendency to bio-molecule (DNA) and possess comparatively high binding constant {Kb) values than the ligands. The DNA binding study indicate partial intercalative mode of binding in complex-DNA. The gel electrophoresis activity was carried out to examine DNA nuclease property of pUC19 plasmid DNA.
机译:具有通式[Pt(LN)C 12]的方形平面单核铂(LL)配合物,用中性双茴香杂环1,3,5-三取代的双吡唑基配体合成。合成化合物的特征是通过物理化学方法,例如TGA,摩尔传导,微型元素分析和磁矩,以及Spectro-Scopic方法,例如FT-IR,UV-Vis,NH NMR,13C NMR和质谱。使用体外盐水虾致死性生物测定进行化合物的生物学应用,体外抗微生物研究,对抗五种不同病原体,以及对Schizosaccaromyces Pombe(5.Pombe)细胞的细胞水平细胞毒性。使用电子吸收滴定,粘度测量研究,荧光猝灭技术和分子对接测定测试Pt(LL)复合物进行DNA相互作用活动。在0.23-1.07×10 5米和0.51-3.13×10 5米^ ^ ^ ^ ^℃下观察到配体和配合物的结合常数{kb)。 Pt(LL)复合物(IIV)显示对生物分子(DNA)的优异结合趋势,并且具有比配体相对高的结合常数(KB)值。 DNA结合研究表明复合DNA中的部分嵌入模式。进行凝胶电泳活性以检查PUC19质粒DNA的DNA核酸酶属性。

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