title: Self-assembly of novel molecular complexes of 1,10-phenanthroline and 5-amino-1,10-phenanthroline and evaluation of their in vitro antitumour activity.
abstract: Novel molecular complexes of 1,10-phenanthroline (phen) and 5-amino-1,10-phenanthroline (5-NH2-phen) [(5-NH2-phen)2(phen) (H2O)3 (1), (phen)2(imidazole) (H+) (BF4-) (2), (phen)2(benzimidazole) (H+) (BF4-) (3), (5-NH2-phen)4(H2O)3 (4), and (phen)3 (indole) (H+) (BF4-) (5)] were synthesized via self-assembly processes and their in vitro anticancer activity was investigated. The structures of the compounds were confirmed by UV, FTIR, CIMS(CH4) and elemental analysis. The crystal structure of 2 was determined by X-ray diffraction. Cytotoxicity of the substances was measured using the cultivated human tumour cell lines HepG2, HEp-2, and 8-MB-GA. The tested substances showed different activity depending on the cell line and amount used. Substances 2 and 3 were not toxic to the non-tumour cells (Lep-3), but significantly toxic to all tumour ones. This is not the case with compounds 4 and 5, which are non-toxic towards carcinogenic cell lines, but even stimulate both HepG2 and HEp-2.
authors.affiliation: Department of Organic Chemistry, University of Chemical Technology and Metallurgy, 8, Saint Kliment Ohridski Blvd., Sofia 1756, Bulgaria. nikolaykaloyanov@yahoo.com
authors.forename: Nikolay
authors.initials: N
authors.lastname: Kaloyanov
authors.forename: Radostina
authors.initials: R
authors.lastname: Alexandrova
authors.forename: Diana W
authors.initials: DW
authors.lastname: Wesselinova
authors.forename: Heike
authors.initials: H
authors.lastname: Mayer-Figge
authors.forename: William S
authors.initials: WS
authors.lastname: Sheldrick
authors.forename: Georgi D
authors.initials: GD
authors.lastname: Dimitrov
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D010618:Phenanthrolines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D010618:Phenanthrolines; C025205:1,10-phenanthroline