Synthesis, characterization, DNA interactions, DNA cleavage, radical scavenging activity, antibacterial, anti-proliferative and docking studies of new transition metal complexes

Abstract

The compound N-(2-hydroxybenzylidene)-1-ethyl-1, 4-dihydro-7-methyl-4-oxo-1, 8 naphthyridine-3-carbohydrazide (LH) and its Cu (II), Co (II) and Zn (II) complexes were synthesized and characterized. The absorption spectral titrations and competitive DNA binding studies depicted those complexes of title compound bind to CT-DNA through intercalation. Interestingly [Cu (II)-(L2)] showed relatively high binding constant value (6.61 x 10(5) M(-1)) compared to [Co (II)-(L2)] (4.378× 10(5) M(-1)) and [Zn (II)-(L2)] (3.1x10(5) M(-1)). Ligand and its complexes were also examined for DNA nuclease activity against pBR-322 plasmid DNA, which showed that [Cu (II)-(L2)] had the best hydrolytic cleavage property displaying prominent double-strand DNA cleavage. In addition, antioxidant activities of the ligand and its metal complexes investigated through scavenging effects for DPPH radical in- vitro, indicated their potentiality as good antioxidants. The in vitro anti-bacterial study inferred the better anti-bacterial activity of [Cu (II)-(L2)] and this was also correlated theoretically by employing docking studies wherein [Cu (II)-(L2)] displayed good Gold score and Chem score. Finally the in vitro anti- proliferative activity of studied compounds was tested against HeLa and MCF-7 cell lines. Interestingly [Cu (II)-(L2)] displayed lower IC50 value and lower percentage of viability in both HeLa and MCF-7 cell lines.

Investigation of antituberculosis, antimicrobial, anti-inflammatory efficacies of newly synthesized transition metal(II) complexes of hydrazone ligands: structural elucidation and theoretical studies

“…Thus, the metal complexes of hydrazone ligand are also broadly studied in medicinal chemistry with the purpose to discover a safe and effective therapeutic drug to cure numerous pathogenic diseases. Literature shows that these metal complexes have numerous pharmaceutical applications such as antimicrobial 6 , anti-TB 7 , 8 , anticancer 9 , 10 , antioxidant 11 , anti-inflammatory 12 , antimalarial 13 etc. Further, the medicinal chemist faces a lot of problems to develop an effective drug with minimal disadvantages, therefore, in silico studies are worth mentioning to overcome these issues.…”

Targeting the molecular chaperone SlyD to inhibit bacterial growth with a small molecule

“…Recent examples include the complexes of [CuX 2 (INH) 2 ]·nH 2 O (X = Cl and n = 1; X = NCS and n = 5; X = NCO and n = 4; INH = isoniazid), which have been optimized for in vitro antibacterial activity 48 . The compound N-(2-hydroxybenzylidene)-1-ethyl-1, 4-dihydro-7-methyl-4-oxo-1, and 8 naphthyridine-3-carbohydrazide and their Cu(II), Co(II) and Zn(II) complexes were synthesized and characterized and their antibacterial activities have been tested under in vitro conditions 49 . Cu(II) complexes with the chemotherapeutic antibacterial norfloxacin and N-donor mixed-ligands have been recently reported 50 .…”