Fluorescence, DNA Interaction and Cytotoxicity Studies of 4,5-Dihydro-1H-Pyrazol-1-Yl Moiety Based Os(IV) Compounds: Synthesis, Characterization and Biological Evaluation

Osmium(IV) pyrazole compounds and ligands were synthesized and well characterised. Ligands were characterized by heteronuclear NMR spectroscopy (H-1 & C-13), elemental analysis, IR spectroscopy and liquid crystal mass spectroscopy. Os(IV) complexes were characterized by ESI-MS, ICP-OES, IR spectroscopy, conductance measurements, magnetic measurements and electronic spectroscopy. Binding of compounds with HS-DNA were evaluated using viscosity measurements, absorption titration, fluorescence quenching, and molecular docking, which show effective intercalation mode exhibited by compounds. Binding constant of Os(IV) complexes are found to be 8.1 to 9.2 x 10(4) M-1. Bacteriostatic and cytotoxic activities were carried out to evaluate MIC, LC50, and IC50. The compounds have been undergone bacteriostatic screening using three sets of Gram(+ve) and two sets of Gram(-ve) bacteria. MIC of complexes are found to be 72.5-100 mu M, whereas that of ligands fall at about 122.5-150 mu M.. LC50 count of ligands fall in the range of 16.22-17.28 mu g/mL whereas that of complexes of Os(IV) fall in the range of 4.87-5.87 mu g/mL. IC50 of osmium compounds were evaluated using HCT-116 cell line. All the Os(IV) compounds show moderate IC50.