Evolution of 1, 3, 5-trisubstituted bipyrazole scaffold based platinum(II) complexes as a biological active agent
| Autor: | Mohan N. Patel, Bharat H. Pursuwani, Miral V. Lunagariya, Khyati P. Thakor |
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| Rok vydání: | 2018 |
| Předmět: |
Electrophoresis
Magnetic Resonance Spectroscopy Denticity Drug Evaluation Preclinical chemistry.chemical_element Platinum Compounds Chemistry Techniques Synthetic 010402 general chemistry 01 natural sciences Biochemistry chemistry.chemical_compound Schizosaccharomyces Spectroscopy Fourier Transform Infrared Genetics Animals Gel electrophoresis Deoxyribonucleases Cytotoxins 010405 organic chemistry DNA General Medicine Carbon-13 NMR Binding constant Combinatorial chemistry Anti-Bacterial Agents 0104 chemical sciences Molecular Docking Simulation chemistry Thermogravimetry Proton NMR Molecular Medicine Spectrophotometry Ultraviolet pUC19 Artemia Platinum |
| Zdroj: | Nucleosides, Nucleotides and Nucleic Acids. 37:455-483 |
| ISSN: | 1532-2335 1525-7770 |
| Popis: | Square planar mononuclear platinum(II) complexes having general formula [Pt(Ln)Cl2], (where, Ln = L1-4) 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, 1H 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 (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 (Kb) of ligands and complexes were observed in the range of 0.23-1.07 × 105 M-1 and 0.51-3.13 × 105 M-1, respectively. Pt(II) complexes (I-IV) display an excellent binding tendency to biomolecule (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. |
| Databáze: | OpenAIRE |
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