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.
The neutral rhenium(I) complexes (I-VI) of type [ReCl(CO) 3 L n ] {where L 1 = 7-phenyl-5-(pyridin-2-yl)pyrazolo[1,5-a] pyrimidine, L 2 = 7-(4-bromophenyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimi-dine, L 3 = 7-(4-chlorophenyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine, L 4 = 7-(2-chlorophenyl)-5-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine, L 5 = 7-(4-methoxyphenyl)-5-(pyridin-2-yl)pyrazolo [1,5-a]pyrimidine, L 6 = 5-(pyridin-2-yl)-7-(p-tolyl)pyrazolo[1,5-a]py-rimidine} were synthesized and characterized by 13 C-APT, 1 H-NMR, IR, electronic spectra, magnetic moment and conductance measurement. The anti-proliferative activity on HCT116 cells by MTT assay suggests potent cytotoxic nature of complexes, some complexes even have better activity than standard drug cisplatin, oxaliplatin, and carboplatin. The complexes were found to have better antimicrobial activity compare to pyrazolo pyrimidine ligands. The theoretical study of compounds-DNA interactions was examined by molecular docking as a supportive tool to the experimental data, which suggests the groove mode of binding. The values of docking energy for compounds-DNA interaction were found in the range of-230.31 to-288.34 kJ/mol. The intrinsic binding constant values of complexes (1.1-3.5 × 10 5 M-1) were found higher than the ligands (0.32-1.8 × 10 5 M-1).
Correction for ‘Synthesis, characterization and biological application of 5-quinoline 1,3,5-trisubstituted pyrazole based platinum(ii) complexes’ by Miral V. Lunagariya et al., MedChemComm, 2018, DOI: ; .
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