Pyrazolone incorporating bipyridyl metallointercalators as effective DNA, protein and lung cancer targets: Synthesis, characterization and in vitro biocidal evaluation

摘要: Pyrazolone based metal complexes have strong bio-activity but the anti-cancer mechanism of these derivatives is not fully understood. In recent years, Cu(II) attracted interest researchers increasingly because their high antitumor activities that are usually related to DNA binding. The reaction three different (I) PPMP [3-methyl-1-phenyl-4-propionyl-1H-pyrazol-5(4H)-one], (II) TMCPMP [1-(3-chlorophenyl)-3-methyl-4-(4-methylbenzoyl)-1H-pyrazol-5(4H)-one] and (III) PPTPMP [3-methyl-4-propionyl-1-p-tolyl-1H-pyrazol-5(4H)-one] 3-methyl-1-phenyl-1H-pyrazol-5(4H)-one 2.2' bipyridyl along with Cu(NO3)2·3H2O under methanolic condition allowed us isolate characterize a series new mixed ligand [Cu(TMCPMP) (Bipy)NCS] (1) [Cu(PPMP) (2) [Cu(PPTPMP) (3). All well characterized by elemental analysis, estimation, molar conductivity, FT-IR UV-Vis spectroscopy. molecular geometry has been determined single crystal X-ray study. single-crystal structures 1 2 exhibit square pyramidal geometry, while complex 3 revealed slightly distorted square-pyramidal geometry. binding compounds Calf-Thymus (CT-DNA) explored emission titration methods, which 1-3 could interact CT-DNA through intercalation mode. also exhibited Bovine Serum Albumin (BSA) over ligands. Complexes were evaluated for in vitro cytotoxic against lung cancer cell lines (A549) as noncancerous rat cardiomyocytes (H9C2) lines, showed all substantial activity minimum effect on cells. Complex more hydrophobic environment relatively towards A549 summary, this belongs class copper-pyrazolonate target many biochemical sites potential activity. results collectively suggested serve promising pharmacologically active substance cancer.