title: Investigation of nuclease, proteolytic and antiproliferative effects of copper(II) complexes of thiophenylmethanamine derivatives.
abstract: Four coordinate copper(II) complexes 1, 2 and 3 of ligands based on thiophenemethylamine containing imidazole, benzimidazole and pyridine moiety have been synthesized and characterized. Complex 1 has also been crystallographically characterized. The three complexes bind to DNA non-intercalatively, though partial intercalation in the case of complex 2 cannot be ruled out. All the three complexes bring about hydroxyl radical mediated DNA cleavage in the presence of H₂O₂. Binding of the three copper(II) complexes to BSA lead to changes in the helicity of the protein. Among the three complexes, 2 and 3 are more effective in inhibiting the growth of cancerous MG63 cells than normal NIH3T3 cells. These two complexes promote apoptosis in MG 63 cells.
authors.affiliation: Chemical Laboratory, Central Leather Research Institute, Council of Scientific and Industrial Research, Adyar, Chennai 600 020, India.
authors.forename: Subramaniyam
authors.initials: S
authors.lastname: Rajalakshmi
authors.forename: Manikantan Syamala
authors.initials: MS
authors.lastname: Kiran
authors.forename: Vaidyanathan Ganesan
authors.initials: VG
authors.lastname: Vaidyanathan
authors.forename: Ettyapuram Ramaprasad
authors.initials: ER
authors.lastname: Azhagiya Singam
authors.forename: Venkatesan
authors.initials: V
authors.lastname: Subramaniam
authors.forename: Balachandran Unni
authors.initials: BU
authors.lastname: Nair
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002417:Cattle; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003300:Copper / Q000737:chemistry*; D018360:Crystallography, X-Ray; D004247:DNA / Q000737:chemistry / Q000187:drug effects*; D053837:DNA Cleavage; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006861:Hydrogen Peroxide / Q000494:pharmacology; D008744:Methylamines / Q000737:chemistry*; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D041681:NIH 3T3 Cells; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D059748:Proteolysis / Q000187:drug effects; D012710:Serum Albumin, Bovine / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D008744:Methylamines; D009942:Organometallic Compounds; D012710:Serum Albumin, Bovine; D003300:Copper; D004247:DNA; D006861:Hydrogen Peroxide
keywords: Copper(II) complexes; Cytotoxicity; DNA and BSA binding/cleavage