European journal of medicinal chemistry · 2012
Mixed-ligand Cu(II)-vanillin Schiff base complexes; effect of coligands on their DNA binding, DNA cleavage, SOD mimetic and anticancer activity.
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Tabassum Sartaj, Amir Samira, Arjmand Farukh, Pettinari Claudio, Marchetti Fabio, Masciocchi Norberto, Lupidi Giulio, Pettinari Riccardo
Аннотация
SOD mimics with varying coligand are momentous in developing potential chemotherapeutic drugs. Cu(II) based SOD mimics 1-4 [CuLH(OAc)(H(2)O)Y)] (LH = 2-((E)-(1,3-dihydroxy-2-methylpropan-2-ylimino)methyl)-6-methoxyphenol, OAc = CH(3)COO, 1: Y = H(2)O; 2: Y = phen (1,10-phenanthroline), 3: Y = tpimH (2,4,5-triphenylimidazole); 4: Y = tfbimH (2-(trifluoromethyl)benzimidazole) were synthesized and thoroughly characterized. Their interaction with CT-DNA showed different non-covalent binding behaviour. SOD activity of 2 was highest among 1-4 which was further validated by gel electrophoresis. The pBR322 plasmid strand break offered by 2 + O₂·⁻ system reveals oxidative cleavage mechanism. In vitro antimicrobial activity of 1-4 was shown by percent inhibition data while in vitro anticancer activity of 1-4 was screened using 16 human carcinoma cell lines of different histological origin. Complex 2 showed higher efficacy towards 14 cell lines.
Предметные рубрики MeSH
Anti-Bacterial AgentsAntifungal AgentsAntineoplastic AgentsAspergillus nigerBenzaldehydesBinding SitesCandida albicansCell Line, TumorCell ProliferationCopperDNADNA CleavageDose-Response Relationship, DrugDrug Screening Assays, AntitumorGram-Negative BacteriaGram-Positive BacteriaHumansLigandsMicrobial Sensitivity TestsModels, MolecularMolecular StructureOrganometallic CompoundsStructure-Activity RelationshipSuperoxide Dismutase