title: Mixed-ligand Cu(II)-vanillin Schiff base complexes; effect of coligands on their DNA binding, DNA cleavage, SOD mimetic and anticancer activity.
abstract: 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.
authors.affiliation: Department of Chemistry, Aligarh Muslim University, UP 202002, India. tsartaj62@yahoomail.com
authors.forename: Sartaj
authors.initials: S
authors.lastname: Tabassum
authors.forename: Samira
authors.initials: S
authors.lastname: Amir
authors.forename: Farukh
authors.initials: F
authors.lastname: Arjmand
authors.forename: Claudio
authors.initials: C
authors.lastname: Pettinari
authors.forename: Fabio
authors.initials: F
authors.lastname: Marchetti
authors.forename: Norberto
authors.initials: N
authors.lastname: Masciocchi
authors.forename: Giulio
authors.initials: G
authors.lastname: Lupidi
authors.forename: Riccardo
authors.initials: R
authors.lastname: Pettinari
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001234:Aspergillus niger / Q000187:drug effects / Q000254:growth & development; D001547:Benzaldehydes / Q000737:chemistry*; D001665:Binding Sites / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003300:Copper / Q000737:chemistry*; D004247:DNA / Q000737:chemistry / Q000187:drug effects*; D053837:DNA Cleavage; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D008024:Ligands; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013482:Superoxide Dismutase / Q000737:chemistry / Q000378:metabolism*
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D001547:Benzaldehydes; D008024:Ligands; D009942:Organometallic Compounds; D003300:Copper; D004247:DNA; C100058:vanillin; D013482:Superoxide Dismutase