Litcius/Paper detail

Tetrazolo[1,5-a]quinoline moiety-based Os(IV) complexes: DNA binding/cleavage, bacteriostatic and photocytotoxicity assay

Bharat H. Pursuwani, Bhupesh S. Bhatt, Foram U. Vaidya, Chandramani Pathak, Mohan N. Patel

2020Journal of Biomolecular Structure and Dynamics12 citationsDOI

Abstract

Biological applications of platinum group metal-based complexes have been widely explored in synthetic and inorganic chemistry. The compounds have been subjected to DNA binding, DNA cleavage, In-vivo and In-vitro photocytotoxicity (HCT-116 cell line) and bacteriostatic activities. Binding constant of complexes are 1.42–5.62 × 104 M−1, whereas that of ligands are 1.12–4.72 × 104 M−1. Ksv of complexes are about 1.32–5.21 × 103 M−1, whereas Kf is about 1.24–6.83 × 103 M−1. IC50 of compounds screened using HCT-116 cell line in dark are found to be 121–342 μg/mL. Whereas photocytotoxicity is found in the range of 48–316 μg/mL. Docking energy of molecules have been evaluated to evaluate efficacy of binding. Molecular docking energy of complexes are in the range of −286.00 to −303.11 kJ/mol. Whereas that of ligands are −254.03 to −282.96 kJ/mol. MIC of complexes are 47 ± 2.5 to 77.50 ± 7.5 μM. LC50 values of ligands fall in the range of 4.05–19.72 μg/mL and that of Os(IV) complexes fall in the range of 3.99–15.99 μg/mL. The Os(IV) complexes dominate in proving its potentiality compared to N, N-donor ligands in biological activities. Communicated by Ramaswamy H. Sarma

Topics & Concepts

ChemistryCleavage (geology)QuinolineMoietyDNAStereochemistryBinding constantIn vitroIn vivoMoleculeMetalBinding siteMedicinal chemistryBiochemistryOrganic chemistryBiotechnologyFracture (geology)BiologyGeotechnical engineeringEngineeringMetal complexes synthesis and propertiesSynthesis of Tetrazole DerivativesSynthesis and biological activity