Evolution of 1, 3, 5-trisubstituted bipyrazole scaffold based platinum(II) complexes as a biological active agent. (3rd August 2018)

• Record Type: Journal Article
• Authors: Lunagariya, Miral V.; Thakor, Khyati P.; Pursuwani, Bharat H.; Patel, Mohan N.
• Is Part Of: Nucleosides, nucleotides & nucleic acids. Volume 37:Number 8(2018)
• Page Start: 455
• Page End: 483
• Publication Date: 2018-08-03
• Subjects: Neutral N -- S –donor bidentate 1 -- 3 -- 5-trisubstituted bipyrazole derivatives ligands -- Pt(II) complexes -- DNA binding study -- Cellular level cytotoxicity -- DNA nuclease activity; Nucleosides -- Periodicals; Nucleotides -- Periodicals; Nucleic acids -- Periodicals; 572.8
• DOI: 10.1080/15257770.2018.1498510
• Languages: English
• ISSNs: 1525-7770

Abstract

Abstract: Square planar mononuclear platinum(II) complexes having general formula [Pt(L n )Cl2 ], (where, L n = L 1–4 ) 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 spectroscopic method such as, FT-IR, UV–vis, 1 H NMR, 13 C 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 ( S. Pombe ) cells. Pt(II) complexes were tested for DNA interaction activities using electronic absorption titration, viscosity measurements study, fluorescence quenching technique and molecular docking assay. Binding constants ( K b ) of ligands and complexes were observed in the range of 0.23–1.07 × 10 5 M −1 and 0.51–3.13 × 10 5 M −1, respectively. Pt(II) complexes (I–IV) display an excellent binding tendency to biomolecule (DNA) and possess comparatively high binding constant ( K b ) 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. Graphical Abstract: