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Eur J Med Chem ; 70: 280-93, 2013.
Article in English | MEDLINE | ID: mdl-24161705

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.


Subject(s)
Antineoplastic Agents/pharmacology , Copper/chemistry , DNA/drug effects , Methylamines/chemistry , Organometallic Compounds/pharmacology , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Cattle , Cell Line, Tumor , Cell Proliferation/drug effects , Crystallography, X-Ray , DNA/chemistry , DNA Cleavage , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Hydrogen Peroxide/pharmacology , Mice , Models, Molecular , Molecular Structure , NIH 3T3 Cells , Organometallic Compounds/chemical synthesis , Organometallic Compounds/chemistry , Proteolysis/drug effects , Serum Albumin, Bovine/chemistry , Structure-Activity Relationship
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